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Shelke, P V
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Medicine & Pharmacology

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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.
Optimization and evaluation of nebivolol hydrochloride loaded transferosomes using Box-Behnken experimental design Shelke, P V; Rachh, Punit R; Mankar, Someshwar; Amin, Saurin; Jain, Deepak
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.v12i4.590

Abstract

Background: This study optimizes and evaluates transferosomes containing Nebivolol Hydrochloride to enhance the drug's bioavailability and therapeutic efficacy. Ultra-deformable vesicles called transferosomes help to increase drug administration via the skin. Methodology: Using a thin-film hydration technique, beta-blocker Nebivolol Hydrochloride, which has antihypertensive properties, was added to transferosomes. To attain the ideal vesicle size (between 200 to 300 nm), entrapment efficiency, and deformability, the formulation was adjusted by adjusting the amounts of phosphatidylcholine, Span 80, and hydration time using a Box-Behnken experimental design. Particle size analysis, zeta potential measurement, and in vitro drug release tests were performed to characterize the transferosomes. Results and discussion: The optimized formulation demonstrated notable deformability, an entrapment effectiveness of 50%, and a vesicle size of 265 nm. The Box-Behnken design made it easier to evaluate the interactions between variables systematically. In vitro drug release studies showed a drug diffusion that persisted for a whole day, suggesting that transferosomes may have long-lasting therapeutic effects. Stability studies at room temperature and accelerated conditions over six months confirmed the formulation's robustness. Conclusion: The results imply that Nebivolol Hydrochloride transferosome-based delivery may be a viable strategy for improving the drug's bioavailability and effectiveness, as nearly 100% of drugs diffuse within 24 hr, perhaps leading to a breakthrough in the management of hypertension.
Co-Authors Amin, Saurin Jain, Deepak Mankar, S D Mankar, Someshwar Prasad L. Gorde Rachh, Punit R