Investigating New Bilosomes for Ex vivo Skin Deposition, In Vitro Characterization, and Transdermal Delivery of Nimodipine

Abstract

Background:This study developed and evaluated bilosomes containing Nimodipine (NDP) to create an appropriate formulation for a sustained-release transdermal gel.The generated bilosomal gel formulation was tested for its potential to increase NDP bioavailability and regulate its release from the transdermal gel dose form.This analysis included ex vivo, in vivo, and in vitro drug release trials. Purpose: The objective of this work was to verify the validity of this notion by creating new nano bilosomes, modifying the composition of existing ones, and employing different bile salts as endogenous agents (EnAs). Subsequently, they sought to evaluate the efficacy of these novel bilosomes in comparison to a drug solution for the transdermal delivery of NDP. Method:To find the best thin film hydration composition, bilosomes used a 33-factor design. This procedure utilizes Design Expert® software.We are creating and testing bilosomes with nimodipine to identify the optimal transdermal gel dose form that delivers the drug slowly and effectively while enhancing NDP bioavailability. We tested the medicine's transdermal gel release control in ex-vivo, in-vivo, and in-vitro trials. Results:The NDP-bilosomes were tuned for a diameter of 136.48±7.82 nm, a surface charge of -48.37±0.49 mV, and an 88.56±1.73% drug encapsulation efficiency Their high negative zeta potential stabilized the compositions. TEM revealed spherical optimized vesicles. Bilosome biphasic NDP release validated Higuchi's theory. FTIR, DSC, and XRD showed that the lipid matrix included all NDP. NDP-Bilosomal gel has good pH, viscosity, consistency, and spreadability. In rats, NDP bilosomal gel showed higher peak plasma concentration and bioavailability than oral nimodipine solution, as indicated by a larger AUC0-∞. Both oral NDP suspension and NDP bilosomal gel had Cmax values of 52.37 and 215.39 μg/mL, respectively, 2 and 16 hours post-delivery. Transdermal bilosomal gel delivery led to increased NDP release, with an AUC0-∞ value of 67.21082238 (g.h/mL).After oral dosage,AUC was 0.439769476 g.h/mL from 0 to infinity (0-∞). The topical safety of F4 was tested on male Wistar rats using in vivo histopathology. Conclusion:Bilosomes were better than drugs for increasing NDP flow over the skin,according to the study. The results showed that bilosomes increase NDP flow and that skin is better than drug solution.