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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 575 journals)
Showing 401 - 253 of 253 Journals sorted by number of followers
Pharmazeutische Zeitung     Full-text available via subscription   (Followers: 11)
Pharmazeutische Industrie     Full-text available via subscription   (Followers: 9)
Pharmaceutical Fronts     Open Access   (Followers: 8)
Advanced Herbal Medicine     Open Access   (Followers: 8)
Pharmaceutical Journal     Free   (Followers: 8)
Drug Metabolism and Pharmacokinetics     Hybrid Journal   (Followers: 6)
Molekul     Open Access   (Followers: 5)
Advances in Pharmacology and Pharmacy     Open Access   (Followers: 5)
AAPS Open     Open Access   (Followers: 5)
Journal of Drug Research in Ayurvedic Sciences     Open Access   (Followers: 4)
Journal of Drug Delivery Science and Technology     Hybrid Journal   (Followers: 3)
Advances in Traditional Medicine     Hybrid Journal   (Followers: 3)
ACS Pharmacology & Translational Science     Hybrid Journal   (Followers: 3)
Canadian Journal of Pain     Open Access   (Followers: 3)
PharmaNutrition     Hybrid Journal   (Followers: 3)
Journal of Pharmacological Sciences     Open Access   (Followers: 3)
Journal of Herbal Science     Full-text available via subscription   (Followers: 3)
Archives of Pharmacy and Pharmaceutical Sciences     Open Access   (Followers: 2)
Advances in Pharmacoepidemiology & Drug Safety     Open Access   (Followers: 2)
Indian Journal of Drugs in Dermatology     Open Access   (Followers: 2)
European Journal of Medicinal Plants     Open Access   (Followers: 2)
Journal of Education and Science     Open Access   (Followers: 2)
Asian Journal of Pharmaceutical Research and Health Care     Open Access   (Followers: 2)
Journal of Herbal Medicine     Hybrid Journal   (Followers: 2)
Current Issues in Pharmacy and Medical Sciences     Open Access   (Followers: 2)
Drug Safety - Case Reports     Open Access   (Followers: 2)
Current Research in Drug Discovery     Open Access   (Followers: 2)
International Journal of Immunopathology and Pharmacology     Open Access   (Followers: 2)
British Journal of Pharmacy (BJPharm)     Open Access   (Followers: 2)
Journal of Pharmaceutical Sciences and Pharmacology     Full-text available via subscription   (Followers: 2)
Psychiatry and Clinical Psychopharmacology     Open Access   (Followers: 1)
Herbal Medicines Journal     Open Access   (Followers: 1)
Journal of Applied Pharmaceutical Research     Open Access   (Followers: 1)
Integrative Medicine International     Open Access   (Followers: 1)
Drugs : Real World Outcomes     Hybrid Journal   (Followers: 1)
Safety and Risk of Pharmacotherapy     Open Access   (Followers: 1)
Regulatory Mechanisms in Biosystems     Open Access   (Followers: 1)
Antiviral Chemistry and Chemotherapy     Open Access   (Followers: 1)
Separation Science plus (SSC plus)     Hybrid Journal   (Followers: 1)
Open Pharmacoeconomics & Health Economics Journal     Open Access   (Followers: 1)
Ethiopian Pharmaceutical Journal     Full-text available via subscription   (Followers: 1)
Journal of the American College of Clinical Pharmacy : JACCP     Hybrid Journal   (Followers: 1)
Advanced Therapeutics     Hybrid Journal   (Followers: 1)
Pharmactuel     Open Access   (Followers: 1)
East and Central African Journal of Pharmaceutical Sciences     Open Access   (Followers: 1)
Journal of Metabolomics & Systems Biology     Open Access   (Followers: 1)
Journal of Pharmaceutical Technology, Research and Management     Open Access   (Followers: 1)
Farmakoèkonomika : Modern Pharmacoeconomic and Pharmacoepidemiology     Open Access   (Followers: 1)
Farmasains : Jurnal Ilmiah Ilmu Kefarmasian     Open Access   (Followers: 1)
Current Research in Pharmacology and Drug Discovery     Open Access   (Followers: 1)
Expert Review of Precision Medicine and Drug Development     Hybrid Journal   (Followers: 1)
OpenNano     Open Access   (Followers: 1)
Emerging Trends in Drugs, Addictions, and Health     Open Access   (Followers: 1)
Journal of Biopharmaceutics Sciences     Open Access   (Followers: 1)
Pediatric Pharmacology     Open Access   (Followers: 1)
Journal of Medicinal Plants for Economic Development     Open Access   (Followers: 1)
Journal of Pharmaceutical Health Care and Sciences     Open Access   (Followers: 1)
Chinese Herbal Medicines     Full-text available via subscription   (Followers: 1)
Pharmakon : Arzneimittel in Wissenschaft und Praxis     Full-text available via subscription   (Followers: 1)
Medicines     Open Access   (Followers: 1)
Future Journal of Pharmaceutical Sciences     Open Access   (Followers: 1)
Pharmacy & Pharmacology     Open Access   (Followers: 1)
Sustainable Chemistry and Pharmacy     Full-text available via subscription   (Followers: 1)
Pharmacological Research - Modern Chinese Medicine     Open Access  
Clinical Complementary Medicine and Pharmacology     Open Access  
Exploratory Research in Clinical and Social Pharmacy     Open Access  
Indonesian Journal of Pharmaceutical Education     Open Access  
Future Drug Discovery     Open Access  
IUPHAR/BPS Guide to Pharmacology CITE     Open Access  
Journal of Applied Pharmaceutical Sciences and Research     Open Access  
Cephalalgia Reports     Open Access  
Pharmacon : Jurnal Farmasi Indonesia     Open Access  
Pharmacia     Open Access  
Research Results in Pharmacology     Open Access  
Journal of Toxins     Open Access  
Journal of Pharmaceutics & Pharmacology     Open Access  
Natural Product Communications     Open Access  
PharmaTutor     Open Access  
International Journal of Pharmaceutical Sciences and Developmental Research     Open Access  
Toxicological Research     Hybrid Journal  
Current Medical Science     Hybrid Journal  
EUREKA : Health Sciences     Open Access  
Iraqi Journal of Pharmacy     Open Access  
Revista Colombiana de Ciencias Químico-Farmacéuticas     Open Access  
Medicine in Drug Discovery     Open Access  
Frontiers in Medical Technology     Open Access  
International Journal of Medical and Pharmaceutical Case Reports     Open Access  
Asian Journal of Research in Medical and Pharmaceutical Sciences     Open Access  
Journal of Pharmaceutical Health Services Research     Hybrid Journal  
AboutOpen     Open Access  
Current Protocols in Pharmacology     Hybrid Journal  
Medical Cannabis and Cannabinoids     Open Access  
Ukrainian Biopharmaceutical Journal     Open Access  
Pharmaceutical Journal of Sri Lanka     Open Access  
Isan Journal of Pharmaceutical Sciences (IJPS)     Open Access  
Ciencia e Investigación     Open Access  
Jurnal Farmasi Sains dan Komunitas (Journal of Pharmaceutical Sciences and Community)     Open Access  
Toxicon : X     Open Access  
International Journal of Pharmaceutics: X     Open Access  
Jurnal Farmasi dan Ilmu Kefarmasian Indonesia     Open Access  
Open Pharmacology Journal     Open Access  
ExRNA     Open Access  
International Journal of Pharmaceutics & Pharmacology     Open Access  
Antibody Therapeutics     Open Access  
Journal of Faculty of Pharmacy of Ankara University     Open Access  
Iraqi Journal of Pharmaceutical Sciences     Open Access  
Journal of Medicinal Botany     Open Access  
Journal of Medicinal Herbs and Ethnomedicine     Open Access  
International Journal of Pharmacokinetics     Hybrid Journal  
Neuropsychopharmacology Reports     Open Access  
Reviews on Clinical Pharmacology and Drug Therapy     Full-text available via subscription  
SynOpen     Open Access  
Matrix Science Pharma     Open Access  
Contract Pharma     Full-text available via subscription  
Journal of Cellular Neuroscience and Oxidative Stress     Open Access  
Istanbul Journal of Pharmacy     Open Access  
Acta Pharmaceutica Indonesia     Open Access  
Indonesian Journal of Pharmacy     Open Access  
EMC - Cosmetologia Medica e Medicina degli Inestetismi Cutanei     Full-text available via subscription  
High-Throughput     Open Access  
Scientia Pharmaceutica     Open Access  
Trends in Peptide and Protein Sciences     Open Access  
Acta Physiologica Hungarica     Full-text available via subscription  
Jurnal Farmasi Sains dan Praktis     Open Access  
Jurnal Kefarmasian Indonesia     Open Access  
Pharmaceutical Historian     Open Access  
Planta Medica International Open     Open Access  
Archives of Razi Institute     Open Access  
Journal of Pharmaceutical Research     Open Access  
EJNMMI Radiopharmacy and Chemistry     Open Access  
FarmaJournal     Open Access  
Journal of Negative and No Positive Results     Open Access  
Pharmaciana     Open Access  
Folia Medica Indonesiana     Open Access  
Актуальні питання фармацевтичної та медичної науки та практики     Open Access  
International Journal of Pharmacology, Phytochemistry and Ethnomedicine     Open Access  
Фармацевтичний часопис     Open Access  
Ciência Equatorial     Open Access  
Iranian Journal of Pharmaceutical Research     Open Access  
Research & Reviews : A Journal of Drug Design & Discovery     Full-text available via subscription  
Asian Journal of Medical and Pharmaceutical Researches     Open Access  
Research & Reviews : A Journal of Pharmacognosy     Full-text available via subscription  
Ars Pharmaceutica     Open Access  
Pharmacognosy Communications     Partially Free  
Egyptian Pharmaceutical Journal     Open Access  
Pharmacological Reports     Hybrid Journal  
PZ Prisma : Materialien zur Fort- und Weiterbildung     Full-text available via subscription  
Chinese Journal of Pharmaceutical Analysis     Full-text available via subscription  
Journal of Nanopharmaceutics and Drug Delivery     Full-text available via subscription  
Journal of Hydrogels     Full-text available via subscription  
Manufacturing Chemist     Full-text available via subscription  
Pharmaceutica Analytica Acta     Open Access  
Journal of Pharmacovigilance     Open Access  
Current Pharmacology Reports     Hybrid Journal  
Nigerian Journal of Natural Products and Medicine     Full-text available via subscription  
International Journal of Herbs and Pharmacological Research     Open Access  
Bangladesh Journal of Physiology and Pharmacology     Open Access  
Research Journal of Pharmacognosy     Open Access  

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Pharmaceutical Fronts
Number of Followers: 8  

  This is an Open Access Journal Open Access journal
ISSN (Print) 2628-5088 - ISSN (Online) 2628-5096
Published by Thieme Publishing Group Homepage  [233 journals]
  • A New Colorimetric DPPH Radical Scavenging Activity Method: Comparison
           with Spectrophotometric Assay in Some Medicinal Plants Used in Moroccan

    • Authors: Babili; Fatiha EL, Nigon, Clotilde, Lacaze, Li, Millé, Juliette, Masiala, Anthony, Simm, Jennifer, Lamade, Virginie M., Haj, Amal Ait El
      Abstract: Antioxidants in medicinal plants are particularly important in protecting against reactive oxygen species (ROS)-related diseases, such as heart and blood vessel disease, nervous system degeneration, and cancer. Because our bodies are not strong enough to completely neutralize ROS, we sometimes need antioxidant supplementation from herbs. There is ample empirical evidence in traditional pharmacopoeias. The antioxidant activities of plant drugs have long been spectrophotometrically measured with 2,2-diphenyl-1-picrylhydrazyl (DPPH). In this study, a new colorimetry DPPH radical scavenging activity method (validated to ICH standards) for some medicinal plants, used in Moroccan pharmacopoeia, was reported and made a comparison with spectrophotometric assay. In the method, a solution of DPPH• is incubated in the presence of an antioxidant control (Trolox) or medicinal plant extracts in wells on a 96-well plate. After an appropriate reaction time, in the dark, the plate was scanned and images obtained were processed and analyzed by Image J software. This analysis will allow us to evaluate substance's antioxidant activity, almost in the same way as a spectrophotometric assay. The colorimetric DPPH• method exhibited a strong correlation (R 2 > 0.95) with the conventional spectrophotometric DPPH• method. The colorimetric DPPH• method had excellent accuracy (103.81–105.47%), precision (1.051–10.85% RSD [relative standard deviation]), reproducibility (1.457% RSD), and robustness (1.05–1.38 F test). The developed DPPH• test was easy, fast, low cost and reliable, and can be used for high-throughput assay for screening DPP-scavenging activity in herb medicines.
      Citation: Pharmaceutical Fronts 2022; 04: e89-e102
      PubDate: 2022-07-09T21:03:13+01:00
      DOI: 10.1055/s-0042-1748031
      Issue No: Vol. 04, No. 02 (2022)
  • Lipid-Based Nanocarrier Systems for Drug Delivery: Advances and

    • Authors: Zhao; Yan-Qi, Li, Li-Jun, Zhou, Er-Fen, Wang, Jiang-Yue, Wang, Ying, Guo, Lin-Miao, Zhang, Xin-Xin
      Abstract: Lipid-based nanocarriers have been extensively investigated for drug delivery due to their advantages including biodegradability, biocompatibility, nontoxicity, and nonimmunogenicity. However, the shortcomings of traditional lipid-based nanocarriers such as insufficient targeting, capture by the reticuloendothelial system, and fast elimination limit the efficiency of drug delivery and therapeutic efficacy. Therefore, a series of multifunctional lipid-based nanocarriers have been developed to enhance the accumulation of drugs in the lesion site, aiming for improved diagnosis and treatment of various diseases. In this review, we summarized the advances and applications of lipid-based nanocarriers from traditional to novel functional lipid preparations, including liposomes, stimuli-responsive lipid-based nanocarriers, ionizable lipid nanoparticles, lipid hybrid nanocarriers, as well as biomembrane-camouflaged nanoparticles, and further discussed the challenges and prospects of this system. This exploration may give a complete idea viewing the lipid-based nanocarriers as a promising choice for drug delivery system, and fuel the advancement of pharmaceutical products by materials innovation and nanotechnology.
      Citation: Pharmaceutical Fronts 2022; 04: e43-e60
      PubDate: 2022-07-04T21:33:53+01:00
      DOI: 10.1055/s-0042-1751036
      Issue No: Vol. 04, No. 02 (2022)
  • Generating a Bispecific Antibody Drug Conjugate Targeting PRLR and HER2
           with Improving the Internalization

    • Authors: Zong; Hui-Fang, Zhang, Bao-Hong, Zhu, Jian-Wei
      Abstract: Antibody drug conjugate (ADC) therapy has become one of the most promising approaches in cancer immunotherapy. The bispecific targeting could improve the specificity, affinity, and internalization of the ADC molecules. Prolactin preceptor (PRLR) and HER2 have crosstalk signaling in breast cancer, and PRLR undergoes a rapid internalization compared with HER2. To improve the efficacy of HER2 ADCs with enhancing the target specificity and internalization, we constructed a PRLR/HER2-targeting bispecific ADC (BsADC). We evaluated the characterization of PRLR × HER2 BsADC from the affinity and internalization, and further assessed its in vitro cytotoxicity in human breast-cancer cell lines (BT474, T47D, and MDA-MB-231) using Cell Count Kit-8 analysis. Our data demonstrated that PRLR × HER2 BsADC kept the affinity to two targeting antigens after conjugating drugs and exhibited higher internalization efficiency in comparison to HER2 ADC. Furthermore, PRLR × HER2 BsADC demonstrated to have superior antitumor activity in human breast cancer in vitro. In conclusion, our findings indicate that it is feasible through increasing the internalization of target antibody to enhance the antitumor activity and therapeutic potential that could be further evaluated in in vivo animal model.
      Citation: Pharmaceutical Fronts 2022; 04: e113-e120
      PubDate: 2022-07-04T21:33:53+01:00
      DOI: 10.1055/s-0042-1749334
      Issue No: Vol. 04, No. 02 (2022)
  • A Novel and Practical Synthesis of Isavuconazonium Sulfate via Anion
           Exchange Resin

    • Authors: Huang; Lei, Zhang, Yi, Chen, Hua, Wang, Wei-Wei, Li, Jian-Qi, Liu, Yu
      Abstract: In this study, an efficient and practical process for the synthesis of isavuconazonium sulfate (compound 1), an antifungal agent, was described. Highlights in the synthesis route are the usage of the ion exchange resin instead of H2SO4 to introduce the HSO4 − anion in the formulation of quaternary ammonium salt (1), and the reaction condition was further optimized to facilitate the scale-up. The overall yield of the process was 57.0% and the high-performance liquid chromatography purity of product was 97.25%, which was higher than that of the reference-listed drug.
      Citation: Pharmaceutical Fronts 2022; 04: e71-e77
      PubDate: 2022-07-04T21:33:50+01:00
      DOI: 10.1055/s-0042-1747641
      Issue No: Vol. 04, No. 02 (2022)
  • Effect of Oxygen and Water on the Stability of Imipenem and Cilastatin
           Sodium for Injection

    • Authors: Zhang; Meng, Liu, Chun-Feng, Chen, Xiao-Yan, Yang, Li-Na, Zhu, Chun-Mei, Teng, Jian-Hao, Wu, Hao-Xiang, Zhang, Fu-Li
      Abstract: The study aimed to investigate the factors affecting the stability of imipenem and cilastatin sodium for injection (IMI/CIL) to improve the quality and stability in IMI/CIL preparation. In this study, the effects of headspace oxygen (HO), water content, particle shape, and particle size on the stability of IMI/CIL were investigated. IMI/CIL was purged with air, premixed oxygen/nitrogen gas (5%/95%), or high-purity nitrogen (99.999%) at 20, 5, or 2% oxygen levels to prepare IMI/CIL with different HO levels. IMI/CIL was stored at 30, 45, and 75% relative humidity for 30 days to prepare IMI/CIL with different water contents. High-performance liquid chromatography method was used for analysis. The results showed that oxygen, water, particle shape, and particle size had significant effects on the stability of IMI/CIL, and free water content is a better predictor of the safety and stability of imipenem and cilastatin sodium than the total water content. The optimization scheme of the above parameters is proposed, which significantly improves the stability of IMI/CIL. This study led to a better understanding of the degradation mechanism of imipenem and cilastatin sodium, and could provide a reference for the selection and control of IMI/CIL process conditions. This study would contribute to the development of IMI/CIL with improved stability.
      Citation: Pharmaceutical Fronts 2022; 04: e78-e88
      PubDate: 2022-07-04T21:33:50+01:00
      DOI: 10.1055/s-0042-1750043
      Issue No: Vol. 04, No. 02 (2022)
  • Synthesis and Biological Evaluation of a Series of Novel
           1-(3-((6-Fluoropyridin-3-yl)oxy)propyl)piperazines as Dopamine/Serotonin
           Receptor Agonists

    • Authors: Du; Xin-Li, Ni, Yan-Na, Ji, Jiang-Rong, Wan, Ze-Hong, Hu, Zhi-Jing, Ge, Yu-Qiang, Li, Jian-Qi, Wang, Guan
      Abstract: Evidence suggested that the use of partial dopamine D2/D3 receptor agonists may be a better choice for the treatment of Parkinson's disease (PD), and the stimulation of 5-HT1A receptors (mainly via nondopaminergic mechanisms) alleviates motor and nonmotor disorders of PD, implying that the multitarget approach may provide a double bonus for the treatment of the disease. In this study, 20 novel 1-(3-((6-fluoropyridin-3-yl)oxy)propyl)piperazine derivatives were designed and synthesized using a bioisosterism approach, and their activities for D2/D3/5-HT1A receptors were further tested. The results showed that several compounds exhibited a multitarget combination of D2/5-HT1A agonism. Compounds 7b and 34c showed agonistic activities on D2/D3/5-HT1A receptor. The EC50 value of 7b for D2/D3/5-HT1A receptor were 0.9/19/2.3 nmol/L, respectively; and the EC50 value of 34c for D2/D3/5-HT1A receptor were 3.3/10/1.4 nmol/L, respectively. In addition, 34c exhibited good metabolic stability (the half-life T 1/2 = 159.7 minutes) in vitro, which is of great significance for the further exploration of multitarget anti-PD drugs.
      Citation: Pharmaceutical Fronts 2022; 04: e9-e21
      PubDate: 2022-03-31T00:00:00+01:00
      DOI: 10.1055/s-0042-1743415
      Issue No: Vol. 04, No. 01 (2022)
  • Design, Synthesis, and Evaluation of Benzoheterocyclic-Containing
           Derivatives as Novel HDAC1 Inhibitors

    • Authors: Jiao; Min-Ru, Han, Bo, Gu, Xiu, Zhang, Hao, Wang, Ai-Ping, Zhang, Qing-Wei
      Abstract: In this study, the synthesis and biological evaluation of a variety of benzoheterocyclic-containing benzamide derivatives were described. Some of these compounds were proved to inhibiting the activity of histone deacetylase 1 (HDAC1) with IC50 values below the micromolar range, retarding proliferation of several human cancer cells, and surprisingly, not possessing toxicity to human normal cells and hERG K+ ion channels. Among those compounds, 3c was the most potent and efficacious derivative. Compound 3c was orally active and displayed excellent in vivo antitumor activity in a HCT-116 xenograft mice model.
      Citation: Pharmaceutical Fronts 2022; 04: e22-e29
      PubDate: 2022-03-31T00:00:00+01:00
      DOI: 10.1055/s-0042-1743487
      Issue No: Vol. 04, No. 01 (2022)
  • Senna podocarpa Emulgel: A Herbal Alternative for Chemical Burn Wound

    • Authors: Isaac; Johnson Ajeh, Daburi, Aisha, Ifeanyi, Benneth, Ben-Umeh, Kenechukwu Chijioke, Adedokun, Abiodun Abigail, Builders, Philip
      Abstract: Senna podocarpa (SP) leaves are used in folk medicines for treatment of burns and wounds as poultices on wound surface. However, to the best of our knowledge, the wound healing ability of this plant has not been scientifically evaluated. This work aimed to determine the wound healing potential of the crude extract of SP leaves, and to evaluate the benefit of its preparation as an emulgel. In this study, the formulations of 2.5% of SP emulgel (F1) and 7.5% of SP emulgel (F2) were prepared by mixing the emulsion phase with the gel phase in a ratio of 1:1, and then physical appearance, globule size, pH, viscosity, swelling, water activity, extrudability, occlusion, spreadability, stability, and wound healing ability were determined. Phytochemical screening showed the presence of alkaloids, saponins, tannins, cardiac glycosides, flavonoids, anthraquinones, and phenols within the hydro-ethanolic extract of SP leaves, and high flavonoid content is believed to be responsible for its healing attributes. Our formulations showed acceptable physical properties. Hematoxylin-eosin and Verhoeff–Van Gieson stain showed that F2 could induce the accumulation of fibroblasts, fibrocytes, inflammatory cells, gland cells, epidermal cells, adipocytes, and collagen in the process of wound healing in mice injured with hydrochloric acid. Encouragingly, the percent of wound contractions in mice treated with F1, F2, and SP leaf poultice were 64, 87, and 50, respectively, suggesting the superior healing properties exhibited by SP emulgel over SP leaf poultice, and this may due to the occlusive property of emulgels. In conclusion, F2 of crude extract of SP leaves has better pharmacological effects on burn and wound healing, and may represent a preferred choice to treat burn wounds in the future.
      Citation: Pharmaceutical Fronts 2022; 04: e30-e39
      PubDate: 2022-03-31T00:00:00+01:00
      DOI: 10.1055/s-0042-1744474
      Issue No: Vol. 04, No. 01 (2022)
  • Novel Docetaxel-Loaded Micelles Based on all-trans-Retinoic Acid:
           Preparation and Pharmacokinetic Study in Rats

    • Authors: Yang; Ya-Ni, Cheng, Jia-Jia, He, Jun, Lu, Wei-Gen
      Abstract: Docetaxel (DTX) is a poorly soluble drug. The purpose of this study was to explore a DTX-loaded micelle delivery system using N-(all-trans-retinoyl)-L-cysteic acid methyl ester sodium salt (XMeNa) as the carrier materials. In this study, amphiphilic surfactant XMeNa was synthesized. Then, the blood biocompatibility and the value of critical micelle concentration (CMC) were assessed by a hemolysis test and pyrene-based fluorescent probe techniques, respectively. The XM-DTX micelles were prepared using the method of thin-film hydration, and characterized by dynamic light scattering and transmission electron microscopy (TEM). The entrapment efficiency (EE) and drug loading efficiency (DLE) were assessed by the ultrafiltration method. In vitro release and pharmacokinetic behaviors of XM-DTX micelles were performed in rats using Taxotere (a commercialized DTX injection) as a control. Our data confirmed the excellent blood biocompatibility of XMeNa as a carrier. XMeNa can self-assemble into micelles in aqueous media with a very low CMC (6.2 μg/mL). The average size and zeta potential of the XM-DTX micelles were 17.3 ± 0.2 nm, and −41.6 ± 0.3 mV, respectively. EE and DLE reached up to 95.3 ± 0.7% and 22.4 ± 0.2%, respectively, which may account for the high solubility of DTX in normal saline. The micelles were spherical in TEM with good dispersion and no aggregation and adhesion, and exhibited good stability after reconstitution over 8 hours. Results from in vitro release assay suggested a much slower release behavior of XM-DTX micelles in comparison to Taxotere. Additionally, XM-DTX micelles prolonged DTX retention in blood circulation, increased the area under the curve by 2.4-fold, and significantly decreased the clearance of the drug. Given above, the XM-DTX micelles could improve the solubility and the release of DTX. The amphiphilic surfactant XMeNa also exhibited great potential as a vehicle for exploring delivery of poorly water soluble drugs in the future.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-09-19T16:07:13+01:00
      DOI: 10.1055/s-0042-1757511
  • Selective Nitro Reduction of Ester Substituted Nitroarenes by NaBH4-FeCl2

    • Authors: Zhou; Zi-Hong, Xu, Yong-Bo, Wu, Shu-Ming, Ling, Wei-Jian, Zhang, Lei, Wang, Zhong-Qing
      Abstract: This work aimed to explore a novel protocol for selective reduction of the nitro group on the aromatic ring while remaining the ester group unaffected. In this study, NaBH4-FeCl2 was disclosed as a key reductant in the process. NaBH4-FeCl2-mediated reduction showed high chemoselectivity, gave the desired products in magnificent yield (up to 96%), and was applied to synthesize a key intermediate of vilazodone (an antidepressant drug) on a hectogram scale in a total yield of 81% (two steps). The protocol is practical, and capable of synthesis of a range of aromatic amines, especially those with ester substituted in the ring.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-09-19T16:07:13+01:00
      DOI: 10.1055/s-0042-1756457
  • The Study of Spray-Freeze-Drying Technique for Development of Novel
           Combination pMDIs, Part I: Study on the Preparation Method

    • Authors: Xi; Quan, Miao, Jia-Ying, Cao, Zhen, Wang, Hao
      Abstract: Clinically available pressurized metered-dose inhalers (pMDIs) mainly directly use micronized drugs as inhalable microparticles. Although technology for preparing pMDIs has proven to obtain clinically appropriate aerosol performance, the fine particle fraction and delivered dose content uniformity (DDCU) of pMDIs still need to be improved. DDCU problem is usually exacerbated by patients' handling errors prior to taking a dose. In this study, novel phospholipid microparticle inhalation pMDIs were prepared by a spray-freeze-drying process using mometasone furoate and formoterol fumarate dihydrate as model drugs and distearoylphosphatidylcholine as an excipient. Combined with the material composition, the atomization and freeze-drying processes were also studied. Our data showed that both atomization parameters of gas–liquid ratio and freeze-drying curve settings met the requirements of drug design. According to aerodynamic performance in vitro and DDCU evaluation, the performance of the phospholipid microparticle inhalation pMDI was better than that of the micronized drug microparticle pMDI. In conclusion, preparing pMDIs with particle engineering has the potential to ensure accuracy of quantification and to improve the efficiency of drug deposition in lungs in clinical practice.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-09-13T13:07:04+01:00
      DOI: 10.1055/s-0042-1755455
  • Enzyme- and Chemo-enzyme-Catalyzed Stereodivergent Synthesis

    • Authors: Lv; Jia-Xiang, Ding, Ya-Qi, Huang, Chen-Ming, Guo, Ling-Ling, Fang, Jia-Li, Jia, Xian, Zhang, Wen-He, You, Song, Qin, Bin
      Abstract: Multiple stereoisomers can be found when a substance contains chiral carbons in its chemical structure. To obtain the desired stereoisomers, asymmetric synthesis was proposed in the 1970s and developed rapidly at the beginning of this century. Stereodivergent synthesis, an extension of asymmetric synthesis in organic synthesis with the hope to produce all stereoisomers of chiral substances in high conversion and selectivity, enriches the variety of available products and serves as a reference suggestion for the synthesis of their derivatives and other compounds. Since biocatalysis has outstanding advantages of economy, environmental friendliness, high efficiency, and reaction at mild conditions, the biocatalytic reaction is regarded as an efficient strategy to perform stereodivergent synthesis. Thus, in this review, we summarize the stereodivergent synthesis catalyzed by enzymes or chemo-enzymes in cases where a compound contains two or three chiral carbons, i.e., at most four or eight stereoisomers are present. The types of reactions, including reduction of substituent ketones, cyclization reactions, olefin addition, and nonredox transesterification reactions, are also discussed for the understanding of the progress and application of biocatalysis in stereodivergent synthesis.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-09-08T07:48:59+01:00
      DOI: 10.1055/s-0042-1755556
  • Generating Anti-TIGIT and CD155 Monoclonal Antibodies for Tumor

    • Authors: Duan; Yu-Hang, Bian, Yan-lin, Zhu, Jian-Wei
      Abstract: Many studies have confirmed that the human poliovirus receptor (PVR; CD155) is related to tumor cell migration, invasion, and thus tumor progression. A PVR receptor binds its ligand T cell Ig and the ITIM domain (TIGIT) to inhibit the function of T and NK cells, thereby allowing tumors to evade immune surveillance. In this study, two IgG1 monoclonal antibodies, anti-CD155 and anti-TIGIT, were expressed by the mammalian transient transfection system, then, antibody-dependent cell-mediated cytotoxicity, antibody-binding affinity, and antitumor efficacy were evaluated subsequently in vitro. In this work, protein A affinity chromatography was used for antibodies' purification. Analysis methods included Western blot, enzyme-linked immunosorbent assay, and flow cytometry. Our data suggested that both the two monoclonal antibodies have a purity of higher than 90%, and bound tightly to the antigen with dissociation constant (K d) and 50% effective concentrations (EC50) below micromolar range. Most notably, these antibodies promote antitumor activity of immune cells in vitro. Therefore, our study laid down the foundation for subsequent in vivo experiments for further evaluation.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-09-02T10:10:48+01:00
      DOI: 10.1055/s-0042-1755454
  • Novel and Practical Industrial Process Scale-Up of
           5-Bromo-2-chloro-4-(methoxycarbonyl)benzoic acid, a Key Intermediate in
           the Manufacturing of Therapeutic SGLT2 Inhibitors

    • Authors: Zhang; Yi, Ma, Xiao, Shan, Xiao-Hui, Zhang, Xiao-Wen, Li, Jian-Qi, Liu, Yu
      Abstract: 5-Bromo-2-chloro-4-(methoxycarbonyl)benzoic acid (1) is a key intermediate for the synthesis of a family of promising SGLT2 inhibitors currently in preclinical and phase I studies for diabetes therapy. In this investigation, cheap, easily available dimethyl terephthalate was used as the raw starting material, and compound 1 was prepared effectively in six steps, including nitration, hydrolysis, hydrogenation, esterification, bromination, and diazotization. The preparation was run successfully on approximately 70 kg/batch with the total yield of 24%. This practical process was demonstrated to be scalable with a great yield and significant cost reduction.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-08-22T14:07:42+01:00
      DOI: 10.1055/s-0042-1755195
  • 3D-QSAR and Docking Studies on Pyrimidine Derivatives of Second-Generation
           ALK Inhibitors

    • Authors: Jiang; Gang-Long, Song, Lian-Hua, Qiu, Yong-Fu, Liu, Yu
      Abstract: Anaplastic lymphoma kinase (ALK) is a promising target for the treatment of non-small cell lung cancer. Under crizotinib treatment, drug resistance and progressive disease appeared after the point mutations arising in the kinase domain of ALK. Second-generation ALK inhibitors can solve the deficiencies of the first generation, especially the drug resistance in cancer chemotherapy. Ceritinib (LDK378), a pyrimidine derivative, for example, can inhibit the activity of ALK with an IC50 value of 40.7 nmol/L, and can experience disease progression after initial treatment with crizotinib. Unfortunately, clear structure–activity relationships have not been identified to date, impeding the rational design of future compounds possessing ALK inhibition activity. To explore interesting insights into the structures of pyrimidine derivatives that influence the activities of the second-generation ALK inhibitors, three-dimensional quantitative structure–activity relationship (3D-QSAR) and molecular docking were performed on a total of 45 derivatives of pyrimidine. Comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) techniques were used to generate 3D-QSAR models. CoMFA and CoMSIA were performed using the Sybyl X 2.0 package. Molecular docking analysis was performed using the Surflex-Dock module in SYBYL-X 2.0 package. We found in the CoMFA model that the non-cross-validated r2 value was 0.998, the cross-validated q 2 value was 0.663, and the F statistic value was 2,401.970, while the r2 value was 0.988; q 2 value was 0.730, and F value was 542.933 in CoMSIA models, suggesting the good predictability of the CoMFA and CoMSIA models. 3D contour maps and docking results suggested that different groups on the core parts of the compounds could enhance the biological activities. Based on these results, the established 3D-QSAR models and the binding structures of ALK inhibitors obtained favor the prediction of the activity of new inhibitors and will be helpful in the reasonable design of ALK inhibitors in the future.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-08-16T15:02:25+01:00
      DOI: 10.1055/s-0042-1750044
  • Structural Characterization of Chemical Compounds Based on Their
           Fragmentation Rules in Sophorae Fructus by UPLC-QTOF-MS/MS

    • Authors: He; Zi-Hui, Liu, Mo, Ren, Jun-Xuan, Ouyang, Dan-Wei
      Abstract: This study aims to identify the chemical components in Sophorae Fructus, and explore the mass spectrometric cleavage rules using the UPLC-Q-TOF-MS/MS method. The main characteristic fragments of the compounds were analyzed by electrospray ionization (ESI) ion source under positive and negative ion modes. The compounds were identified by molecular formula, multistage mass spectrometry, ultraviolet spectrum, and the fragmentation patterns of standards. A total of 142 compounds were identified, including 68 flavonoids, 39 saponins, 21 organic acids, and 14 others, of which 43 components were reported from Sophora for the first time. Moreover, the mass spectrometric fragmentation rules of some identified species components were deduced, which are helpful for the structural analysis of flavonoid and saponins. This method provides a reference for the rapid identification of chemical components and is conducive to further study the pharmacodynamic material basis and action mechanism of Sophorae Fructus.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-08-15T20:37:36+01:00
      DOI: 10.1055/s-0042-1751315
  • Industrial-Scale Preparation of a Key Intermediate for the Manufacture of
           Therapeutic SGLT2 Inhibitors

    • Authors: Huang; Lei, Zhang, Yi, Shan, Xiao-Hui, Liu, Yu, Li, Jian-Qi
      Abstract: (3R,4S,5R,6R)-3,4,5-tris(benzyloxy)-6-methyltetrahydro-2H-pyran-2-one (1) is a key intermediate for the preparation of promising SGLT2 inhibitors currently undergoing clinical tests for diabetes therapy. However, fewer reports have demonstrated the preparation of compound 1 at an industrial scale. In this article, an efficient preparation of the intermediate for the industrial production was explored from commercially available methyl-α-D-glucopyranoside in seven steps, including TBS protection, benzyl protection, TBS removal, iodination, reduction, demethylation, and oxidation. The batch of the validation process was 42.82 kg with a HPLC purity of 99.31%. The main advantages of this approach are that the total cost is lower than the reported laboratory-scale synthetic method, the quality is reproducible, and the process is safe and environmentally friendly.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-08-03T09:23:45+01:00
      DOI: 10.1055/s-0042-1750423
  • Synthesis and Characterization of Related Substances of Torasemide

    • Authors: Chen; Jiong, Ming, Wei, Fan, De-Hua, Gu, Shuang-Xi
      Abstract: Torasemide, a pyridine-3-sulfonylurea derivative, is a high-efficiency loop diuretic. During the process development of torasemide, five process-related substances, which have been specified in the pharmacopeia, would be produced. In this study, all these related substances, including compounds A–E, were synthesized via simple procedures and subsequently characterized by 1H nuclear magnetic resonance (NMR), 13C NMR, and mass spectrometry. Particularly, a simple synthetic method for compound A has not been found in previous literature. It is worth noting that other related substances could be prepared from compound B in one or two steps. The availability of these related substances could allow for quality control in the process of torasemide.
      Citation: Pharmaceutical Fronts ; : -
      PubDate: 2022-06-30T14:48:43+01:00
      DOI: 10.1055/s-0042-1749327
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