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Journal of Applied Pharmaceutical Research
Published by Creative Pharma Assent
ISSN : -     EISSN : 23480335     DOI : 10.18231
Core Subject : Health,
Medicine & Pharmacology
Journal of Applied Pharmaceutical Research (JOAPR) is an official publication of Creative Pharma Assent (CPA). It is an open access, peer review online international journal. JOAPR is primarily focused on multiple discipline of pharmaceutical sciences (Pharmaceutics, Pharmaceutical Technology, Biopharmaceutics, Cosmetic Technology, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy and Phytochemistry, Herbal drugs/ formulations, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest) which publish quarterly. JOAPR also includes evaluation of pharmaceutical excipients & their practical application to research & industry based efforts. The aim of the scientific journal, JOAPR is to present a wide area for the current researchers to share their noble works and ideas in terms of the research papers, review articles and short communications. JOAPR only publish the original research works with a definite innovation and novelty after thorough reviewing. The paper must have a suitable and proper scientific background.
Arjuna Subject : -
Articles 459 Documents
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Precision drug delivery through methotrexate and tofacitinib citrate encapsulated mesoporous silica scaffold Chakole, Dinesh; Rakte, Amol; Pande, Vishal; Kothawade, Sachin; Suryawanshi , Jayprakash
Journal of Applied Pharmaceutical Research Vol. 12 No. 3 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i3.528

Abstract

Background: Advancements in drug delivery aim to enhance outcomes while reducing adverse effects. Mesoporous silica nanoparticles (MSN) offer potential for targeted delivery due to their unique properties, including ordered pore structure, large surface area, and biocompatibility. Methods: MSN were synthesized using tetraethyl orthosilicate (TEOS) and Pluronic F127, then amine-functionalized with 3-aminopropyltriethoxysilane. Methotrexate and tofacitinib citrate were loaded via incipient wetness impregnation. Characterization included FTIR, particle size analysis, TEM, SEM, DSC, XRD, and BET analysis. Results: FTIR confirmed surface modification. Particle size analysis showed nanoscale dimensions. TEM and SEM depicted ordered mesoporous structures. DSC indicated drug crystallinity and MSN amorphism. XRD revealed reduced drug crystallinity in MSN. BET analysis demonstrated high MSN surface area and pore volume. Drug-loading efficiency was 62.44%. Conclusion: Comprehensive synthesis and characterization of MSN for targeted drug delivery were achieved successfully, highlighting their potential in overcoming conventional therapy limitations.
Modulation of mesalamine release from enteric-coated matrix tablets using natural polysaccharides for localized colonic delivery Sahu, Shilpa; Choudhury, Prasanta Kumar; Pasa, Gourishyam; Murthy, Padala Narasimha; Sahu, Poonam; Verma, Renuka
Journal of Applied Pharmaceutical Research Vol. 12 No. 2 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.18231/j.joapr.2024.12.2.93.108

Abstract

Background: Inflammatory bowel diseases (IBD) require effective colon-targeted drug delivery for improved therapeutic efficacy and minimized systemic side effects. Objectives: The objective of this research was to develop and evaluate novel colon-targeted matrix tablet formulations of mesalamine (5-aminosalicylic acid) for the treatment of IBD. Materials and Methods: Mesalamine matrix tablets were prepared by wet granulation technique using pH-sensitive polymers (HPMC K4M) and biodegradable natural polysaccharides (pectin, chitosan, and guar gum). Tablets were characterized for physicochemical properties, drug content, and in vitro drug release. Compatibility studies using FTIR and DSC confirmed no interaction between mesalamine and polymers. The optimized formulations were enteric-coated with Eudragit S100 and ethyl cellulose. Drug release kinetics and stability studies were conducted. Results and Discussion: The uncoated formulations (M3, M6, M7) showed adequate protection against drug release in simulated gastric (0-2 h) and intestinal (2-5 h) fluids. The enteric-coated formulations (ME3, ME6, ME7) exhibited a lag time of around 2 hours and restricted drug release (<5%) in simulated gastric and intestinal fluids up to 5 hours. However, in simulated colonic fluid (pH 6.8) containing 4% rat cecal contents, these formulations showed enhanced drug release (71-83% in 12 h) due to biodegradation of polymeric matrices by colonic enzymes. Drug release kinetics indicated anomalous transport or super case-II transport mechanisms. Stability studies at 40°C/75% RH for 3 months revealed no significant changes. Conclusion: The developed colon-targeted mesalamine matrix tablets demonstrated the potential to protect the drug from release in the upper GIT while facilitating targeted drug delivery to the colon, which could improve therapeutic efficacy and minimize systemic side effects in the treatment of IBD.
Optimizing novasomes: impact of oleic acid and co-surfactant ratio on posaconazole delivery: In vitro & Ex vivo pharmacokinetic study Rukari, Tushar; Pingale, Prashant L; Upasani, Chandrashekhar D
Journal of Applied Pharmaceutical Research Vol. 12 No. 3 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i3.536

Abstract

Background: Posaconazole, currently available as a solid oral dosage form, possesses erratic pharmacokinetics that complicate dosing regimens and increase the risk of adverse effects and drug interactions. Hence, innovative strategies, especially topical ones, are necessary to enhance the therapeutic profile and improve patient outcomes. Methodology: The regular 23 factorial design and the concentrations of Oleic acid: Span 80 (2:1) ratio, Cholesterol, and Tween 80 as independent variables were used for the formulation development. The preliminary effect was determined by dependent variables like vesicle size and entrapment efficiency; then the final optimized batch was loaded in 3 % w/w Carbopol gel. Result and Discussion: The optimized batch's vesicle size and entrapment efficiency were 193.34+14.84 nm and 90.03+0.11 %, respectively. These results were found statistically significant (ANOVA) in the trial version of Stat-Ease 360®. Other evaluation parameters like zeta potential and pH of all the formulations were also significant (p<0.005). Conclusion: The optimized batch (NF7), when loaded with gel (NF7G-3), showed sustained release of Posaconazole up to 7 h in an In vitro diffusion study facilitated 87.14±0.11 % release confirming non-Fickian or Anomalous diffusion, interpreted from Korsmeyer Peppas (KKP) model. With the results from In vitro and Ex vivo pharmacokinetic release, the Posaconazole-loaded NF7G-3 Novasomal gel can exhibit potential formulation for the topical treatment of fungal infections. It will help significantly mitigate the negative effects of Posaconazole.
Formulation and evaluation of ointment containing hydroalcoholic extract derived from the bark of Moringa oleifera for wound healing activity in rat model Sahu, Himanshu; Satapathy, Trilochan; Chandrakar, Shashikant; Gupta, Puahpa Prasad; Sahu, Poonam; Sahu, Akhilesh
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.556

Abstract

Background: This study aimed to assess the effectiveness of a hydroalcoholic extract derived from the bark of Moringa oleifera in facilitating the healing process of second-degree burns wounds. Moreover, a comprehensive assessment was carried out on standardized M. oleifera bark to ascertain its physiochemical characteristics, botanical compound layout, and antioxidant activity, all of which play a crucial role in its capacity to facilitate the healing process of burns. Methods: For 14 days, the efficacy of ointments containing a hydroalcoholic extract of M. oleifera bark at concentrations of 5% and 10% was evaluated for treating second-degree burns in rats. Additionally, histological analysis was conducted on skin tissue samples. Results: The M. oleifera bark extract exhibited TPC (52.56 mg/gm of dried extract) and TFC (84.33 mg/gm of dried extract) value along with antioxidant activity (IC50 value of 0.98 µg/ml) for radical scavenging, in the presence of several phytochemicals. The most favorable outcomes were achieved using a 10% ointment composition, demonstrating a wound closure and tissue repair rate of 83.04 ± 0.89%, along with a noteworthy decrease in tissue oxidative stress indicators. Histological investigations have verified the wound-healing properties of M. oleifera bark extract. Conclusion: Due to its significant antioxidant properties and its capacity to create a moist environment for wounds, M. oleifera has the potential to serve as a natural treatment for burns. Additional clinical trials are recommended to validate the efficacy of M. oleifera bark extract as a therapeutic agent for wound healing.
Exploring the potential of carbocisteine loaded microparticulate system by using ccd model for the treatment of respiratory infections Rane, Bhushan R.; Gavit, Mayur R; Patil, Vaibhav L; Mhatre, Nandini R; Jain, Ashish S
Journal of Applied Pharmaceutical Research Vol. 12 No. 3 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i3.562

Abstract

Background: Multi-particulate drug delivery systems (microbeads) deliver drugs over an extended period, distributing them evenly throughout the gastrointestinal tract and minimizing local irritation. Microbeads are small, solid, free-flowing particulate carriers that contain drug particles that have been dispersed and are either crystalline in solution. Aim: The present work explores the potential of the carbocisteine-loaded floating microparticulate drug delivery system. Methodology: Floating microbeads were prepared using the ionotropic gelation method and optimized using Central Composite Design. Result and discussion: Floating microbeads of prepared carbocisteine were evaluated for the FTIR study, which reveals no interaction between the drug and other excipients. Buoyancy time, drug content, particle size, and % drug release were also characterized; it found that drug release was 90.24 %, up to 17 hours, 250 to 220 µm, and drug content 96.67%, respectively, for the optimized batch. An accelerated stability study was performed, showing that the formulation was stable. Floating microparticulate drugs were prepared, and batch B-3 was optimized based on in-vitro buoyancy and release patterns. The floating ability of the beads was observed visually for 10 to 17 hr, and an increase in polymer concentration decreased the swelling of the beads. Conclusion: The results obtained from the formulation batch B-3 show good results for all the parameters tested. Floating microbeads could be the best possible approach to deliver drugs with the benefit of reduced dosing frequency
Treatment with Terminalia chebula (retz.): possible mechanism of inhibition of spermatogenesis and fertility in albino mice Gupta, Prakash Chandra; Yadav, Laxmi
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.570

Abstract

Background: There has been a continued effort to develop an effective male contraceptive of plant origin due to its ready availability, cost-effectiveness, and fewer side effects.  The present study has evaluated the mechanism of inhibitory action of Terminalia chebula Retz. (T. chebula; family: Combretaceae) on spermatogenesis and fertility in albino mice after oral administration of the aqueous bark extract (100, 300, and 500 mg/kg BW daily) of T. chebula for 35 d. Methodology: The effects of the Terminalia treatment on various reproductive endpoints such as sperm parameters, testis histology, activities of 3ß- and 17ß-HSDs, immunoblot expressions of StAR and AR proteins, immunostaining of AR, serum testosterone level, LPO level, activities of SOD and catalase, and fertility indices were investigated. Toxicological and recovery studies have also been performed. Results: Testes in Terminalia-treated mice showed nonuniform histologic alterations. Sperm parameters, activities of 3ß- and 17ß-HSDs, immunoblot expressions of StAR and AR proteins, immunostaining of AR, and serum testosterone level were adversely affected, though activities of SOD and catalase were unchanged. Libido remained unaffected, but fertility was inhibited markedly in treated males without signs of toxicity. By 42 d of treatment discontinuation, Terminalia-induced deviations in the reproductive endpoints recovered to control levels. Conclusion: The results of the present study indicate that T. chebula treatment reversibly inhibits spermatogenesis and fertility without signs of toxicity. Further, antifertility effects result from diminished production of testosterone due to Terminalia-mediated inhibition of testicular steroidogenesis.
Formulation and in-vitro anticancer activity of nilotinib immediate release and ibrutinib sustained release pellets Gupta, Vishal; Gupta, Jitendra
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.571

Abstract

Background: Blood cancer is a significant contributor to mortality rates worldwide, and its prevalence is projected to rise on a global scale. This trend places considerable strain on healthcare systems and necessitates the expedited development of innovative treatments by pharmaceutical firms to remain competitive. Conventional pellets produce rapid plasma drug levels, but they might cause side effects, decrease effectiveness, and lead to poor therapeutic management. Ibrutinib and Nilotinib are employed to treat leukemia patients. Methodology: The current research aims to formulate, characterize, and anticancer effect of Nilotinib immediate release (NIR) and Ibrutinib sustained release (ISR) seal sugar-coated pellets. Micrometric properties estimated the characterization of the drug pellets, and surface morphology was estimated using scanning electron microscopy. Drug excipient compatibility studies, stability studies, and in-vitro drug release were accessed. Result & Discussion: The results of pellet formulations FNI-1 to FNI-5 showed that FNI-5 formulations showed 100±6.0 µm size and possessed excellent mechanical strength for giving pellets a good self-life; also, due to the higher drug content up to 99%, FNI-5 was the best suited for pellet formulation and because NIR showed 99.18 ± 2.12 drug release at 2h and ISR 99.03±3.74% up to 12h so that anticancer concentration maintained for prolonged period. The standard dose for cytotoxicity against the THP-1 cell line of Nilotinib was found to be 200 mg, and the maintenance oral dose of Ibrutinib was 140mg, with four times the intake of the drug up to 560 mg.  In an in vitro study in FNI-5 (final formulation), the dose of Ibrutinib was reduced to 420 mg. Conclusion: A synergistic effect of Ibrutinib and nilotinib drugs was observed in the inhibition of cancer cell growth, with an IC50 value of 4.585 µg/mL
Microscopic, pharmacognostic and phytochemical evaluation of Sesbania grandiflora leaves Sharma, Sharad; Semwal, Bhupesh Chander; Mazumder, Avijit
Journal of Applied Pharmaceutical Research Vol. 12 No. 3 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i3.577

Abstract

Objective: Sesbania grandiflora is a short-lived and fast-growing edible ornamental plant belonging to the Fabaceae family. Due to its unique therapeutic characteristics such as anti-inflammatory, antitumor, neuroprotective antioxidant, etc., it is utilized as an herbal medication in the Indian traditional medical system to treat various diseases. Therefore, the objective of the current investigation was to offer certain beneficial information regarding the standardization and identification of S. grandiflora leaf, which may be helpful in terms of its validity, purity, and quality. Methods: The micro- and macroscopical study of fresh and dried leaves of Sesbania grandiflora was investigated. Physicochemical parameters were performed according to WHO-recommended parameters. The dried leaves were powdered and extracted with different solvents in a Soxhlet apparatus. The concentrated extract was further used for physiochemical and phytochemical studies. Result:  The fresh leaves of S. grandiflora were examined for their organoleptic characteristics. The leaves are regular compound and pari-pinnate with an average length of 15–30 cm long with green color. The transverse section of the leaf demonstrated the presence of spongy and palisade type of mesophyll cells. Stomata are anxiolytic and anisocytic stomata. Furthermore, Powder microscopy revealed the presence of simple epidermal hairs, dark yellowish-brown tannin fragments, light yellowish resinoids, oil globules, mucilage cells, and spiral vessels. Phytochemical screening revealed the presence of triterpenes, glycosides, tannins,  flavonoids, gallic acid, biotin, and rutin. Conclusion: This study adds to the body of knowledge regarding the standardization and identification of the subject matter and facilitates future research on the Ayurvedic medical system.
Optimization and evaluation of transdermal delivery system for nebivolol hydrochloride Shelke, P V; Rachh, Punit R; Mankar, S D; Prasad L. Gorde
Journal of Applied Pharmaceutical Research Vol. 12 No. 3 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i3.580

Abstract

Background: Nebivolol hydrochloride, a β1-receptor antagonist known for its antihypertensive properties, boasts a plasma half-life of 10 hours and an oral bioavailability of 12%. In this study, we aimed to enhance the therapeutic effectiveness of Nebivolol hydrochloride and circumvent its extensive hepatic first-pass metabolism by developing transdermal matrix patches. Methodology: Utilizing Central Composite Design (CCD), nine formulations were devised, comprising Hydroxypropyl methylcellulose K15M and Eudragit S100 as independent variables, with 10% w/w triethyl citrate as the plasticizer. Key dependent variables were evaluated, including folding endurance, moisture content, tensile strength, in vitro drug release, and flux. Fourier transform infrared spectroscopy (FTIR) assessed the compatibility between the drug and polymer. Results and discussion: Among the formulations, FP8 demonstrated the highest drug release (85.88% over 24 hours), attributed to its elevated concentration of hydrophobic polymer. The optimized formulation was determined based on the results of dependent variables. Conclusion: These findings suggest that the developed matrix transdermal film holds promise as a potential candidate for sustained drug release over a 24-hour.
Optimizing irbesartan spherical agglomerates through principal component analysis and experimental design Gorde, V. D.; Rachh, Punit R.; Mankar, S. D.; Amin, Saurin
Journal of Applied Pharmaceutical Research Vol. 12 No. 3 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i3.581

Abstract

Background: This study explores the amalgamation of crystallization and agglomeration through spherical crystallization, aiming to develop the spherical crystals of Irbesartan with improved micromeritic properties. The main objective is to use spherical crystallization techniques to improve the micromeritic characteristics of Irbesartan, which has poor flow and compressibility because of its crystal habit. Methodology: A solvent change approach was utilized to synthesize spherical agglomerates of Irbesartan. Several system parameters, including the amount of bridging liquid, the rate of stirring, and the concentration of the polymer, were tuned to enhance the particle size distribution and mechanical qualities. SEM, GC, PXRD, DSC, and FTIR analyses characterised the spherical crystals. Result and Discussion: The study demonstrated that spherical crystallization significantly enhanced Irbesartan's micromeritic properties. The angle of repose of optimized agglomerates was reduced by around 52%, indicating improved considerably flowability of irbesartan. The sphericity of the crystals was validated by SEM examination (shape factor: 0.996), and the solvent levels were found to be within allowable bounds by GC analysis. PXRD data showed no polymorphism alterations, and DSC/FTIR analyses confirmed that the excipients and drug were compatible. Conclusion: This process provides a feasible alternative to classic granulation and agglomeration procedures, resulting in better flow, compressibility, and spherical crystals. It streamlines the Irbesartan formulation, improving efficiency and uniformity, reducing manufacturing costs, higher tablet consistency, and enhancing patient compliance.

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