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Journal : Journal of Applied Pharmaceutical Research

Pharmacophore insights and molecular docking of ciprofloxacin analogues against 2XE1: strategies for reduced antibiotic resistance Katlaria, Sanjana; Chauhan, Ashish Singh; Kumar, Krishna; Kumar, Mohit; Chauhan, Bhumika; Jakhmola, Vikash
Journal of Applied Pharmaceutical Research Vol. 12 No. 6 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i6.660

Abstract

Background: Antibiotic resistance is a silent pandemic disease that is growing and causing a global threat. Existing antibiotics are less effective against infectious diseases, so we must discover more potent and effective drugs. The latest report from the World Health Organization (WHO) underscores the global nature of the situation, revealing that high levels of antibiotic resistance in bacteria worldwide lead to life-threatening bloodstream infections and resistance to treatment. Methods: This study focuses on the Molecular Docking and Pharmacophore Modeling of Ciprofloxacin and its analogs to explore ligand-protein interactions and identify potent drugs against AMR. Twenty ciprofloxacin analogs, designed using ChemDraw Pro12.0, were docked with the 2XE1 protein. Molecular docking assessed the binding affinity, with Arguslab 4.0 scoring the lowest docking scores to indicate strong interactions and biological activity. Pharmacophore modeling identified essential molecular features like HBA, HBD, and AI for optimal biological activity. Results: The computational screening identified several compounds with improved binding properties, showing greater affinity towards ALA129, TYR149, and PHE88 amino acids, essential for biological activity. Conclusion: The study identifies the best analog of ciprofloxacin, which can effectively combat antibiotic resistance. Compound 13 showed promising docking scores and relevant pharmacophoric features, outperforming the parent ciprofloxacin in binding affinity, suggesting it could be a potent drug candidate against AMR.
Nanostructured lipid carriers (NLCs): A comprehensive review of drug delivery advancements Panwar, Pramesh; Kumar, Saurabh; Chand, Pallavi; Chauhan, Ashish Singh; Jakhmola, Vikash
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.676

Abstract

Background: Nano-structured lipid carriers (NLCs) have emerged as a significant advancement in lipid-based drug delivery systems. Compared to Solid Lipid Nanoparticles (SLNs), NLCs offer improved drug loading capacity, stability, and controlled release profiles. Objective: This review article explores the structural and functional benefits of NLCs, their enhanced bioavailability, and their potential in targeted therapeutic agent delivery. Methodology: We investigated the unique combination of solid and liquid lipids in NLCs, which creates an internal structure for improved drug encapsulation and sustained release. Various methods were analyzed for their contribution to NLC efficacy, including high-pressure homogenization and solvent emulsification. Results and Discussion: NLCs demonstrated encapsulation efficiency ranging from 85–95%, with particle sizes between 100–300 nm. Drug release was sustained over 24 hours, affirming their effectiveness in controlled drug delivery. Applications of NLCs were highlighted across diverse delivery modes, including topical, pulmonary, oral, parenteral, and ocular. Challenges such as scaling production, overcoming biological barriers, and ensuring regulatory compliance were also addressed. Conclusion: NLCs present a promising future in pharmaceutical sciences, with the potential to improve therapeutic outcomes in complex diseases like cancer and neurodegenerative disorders. Continued research into NLC formulations is critical for advancing patient outcomes and addressing global health challenges.
Advancements in formulations and technologies for colon-targeted drug delivery Rana, Ritik Singh; Ale, Yogita; Pant, Pankaj; Kukreti, Neha; Jakhmola, Vikash
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.825

Abstract

Background: Colonic administration of drugs may enhance drug absorption, reduce adverse reactions, and facilitate delivery to specific therapeutic targets. Objective: Delivering pharmaceuticals to the colon poses challenges that require innovative formulation strategies. Methodology: Various formulation approaches have been explored for colon-targeted drug delivery systems. These approaches target the colon using formulation components that interact with GI physiology parameters such as pH, colonic flora, and enzymes. Result and Discussion: The article discussed the various research studies conducted for colon targeting involving novel strategies such as pH-dependent, enzyme-dependent, Ligand-Receptor-based, new technologies, Phloral, and magnetically derived approaches. It also explored the translational technologies, such as in vivo, in vitro, and in silico, which expedite the transition from fundamental research to clinical application and enhance therapeutic outcomes. Conclusion: In conclusion, the most relevant preclinical studies, encompassing in vitro, in vivo, and in silico research, are delineated to facilitate the strategic advancement of novel colon-targeted therapeutics.
Development and evaluation of an amorphous solid dispersion-based probucol immediate-release tablet Adhikari, Vaibhav; Butola, Mansi; Jakhmola, Vikash; Ojha, Abhijeet; Negi, Arvind
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.997

Abstract

Background: In its crystalline form, probucol has an extremely low bioavailability and is a poor water-soluble drug. The main aim of this study was to enhance the solubility and dissolution rate of probucol by using a solvent evaporation method to develop a solid dispersion that contains polyvinyl pyrrolidone K30 (PVP-K30) and polyethylene glycol 6000 (PEG 6000). Methodology: The solvent evaporation method is considered superior to other techniques for preparing solid dispersions due to its ability to achieve uniform drug distribution at the molecular level. This method ensures homogeneity by dissolving the drug and carrier in a common solvent, reducing the risk of drug recrystallization and enhancing solubility and bioavailability. Result: The drug-to-carrier ratio is the determining factor for dissolution enhancement. The FTIR spectra do not suggest any chemical interaction between PVP-K30 or PEG 6000. The immediate release profiles of both formulations were favourable, with F3 releasing approximately 95.31% of the drug and F6 releasing around 86.77% within 2 hours. This indicates a rapid drug dissolution, which is beneficial for achieving a fast onset of action and enhancing bioavailability.  Conclusion: The solid dispersion formulations F3 & F6 successfully transformed crystalline probucol to an amorphous state, enhancing solubility & dissolving rates appropriate for immediate-release tablets.
Therapeutic potential of bioconstituents in the prevention and treatment of rheumatoid arthritis Morris, Srishti; Srivastava, Yashashvi; Kartikey Kumar; Jakhmola, Vikash
Journal of Applied Pharmaceutical Research Vol. 13 No. 3 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i3.847

Abstract

Background: Rheumatoid arthritis (RA), a joint disease characterized by inflammation and an autoimmune response, affects approximately 1% of the global population. The disruption of immunological tolerance causes the immune system to attack self-molecules, resulting in autoimmune disease. RA is characterized by synovial swelling, accompanied by morning stiffness and joint soreness. Methodology: Herbal pharmacotherapy is now a meaningful focus in the treatment of rheumatoid arthritis. Medicinal plants contain strong active components like flavonoids, alkaloids, stilbenoids, tannins, and sesquiterpene lactones. Their anti-inflammatory and antioxidant qualities make them a potential treatment option for RA. Results and Discussion: Standard medication aims to prevent further deterioration of the affected joint. This treatment includes several antirheumatic medications, such as methotrexate, biological agents, cytotoxic drugs, immunosuppressants, and NSAIDs. Urinary and respiratory tract infections have been reported in patients treated with certolizumab pegol. Several concerns regarding anti-rheumatoid medication arise during a woman's pregnancy. Therefore, rheumatoid arthritis is now being effectively treated with herbal pharmacotherapy. Conclusion: RA is a chronic autoimmune disorder that primarily affects joints through persistent inflammation. Conventional treatment regimens for RA can lead to the occurrence of adverse effects, such as urinary and respiratory tract infections. Given these challenges, herbal pharmacotherapy is emerging as a safer and more sustainable approach. This review highlights a variety of phytochemicals with anti-inflammatory and antiarthritic properties, including flavonoids, alkaloids, stilbenoids, tannins, and sesquiterpene lactones. It underscores the need for further research to elucidate their mechanisms of action, assess their long-term safety and clinical utility, and compare their efficacy.