Ursolic Acid Loaded Transniosomes Nanogel for Topical Delivery: Statistical Optimization with Box-Behnken Design of Quality by Design (QbD), in vitro and Dermatokinetic Evaluation

Abstract:

Aim: The current research was performed for the preparation and optimization of Transniosomes (TN) preparation for the dermic distribution of Ursolic Acid (UA). Materials and Methods: The formulation was optimized by using the “Box–Behnken design” software. Particles size, % EE, and in vitro study was performed for the optimal formulations after they had been optimised. In addition, morphological, CLSM and dermatocokinetic studies were performed in order to complete the evaluation of the optimal formulation of TN. Results: The improved UA-TN formulation showed vesicles in the shape of lamellae that were completely sealed, with particles size, percentage EE and in vitro release of 145.5 ± 2.56 nm, 84.74 ± 2.49% and 86.28 ± 1.74%. respectively. The percentage cumulative drug permeated through skin for UA-CF gel and UA-TN gel was 36.30% and 84.05% respectively. When equated to the Rhodamine B-hydro methanolic liquid, the confocal pictures that were acquired of rat skin evidently demonstrated that the loaded rhodamine B with TN gel formulation allowed for a deeper penetration of the substance. Further, the UA-TN gel applied mice skin disclosed significant changes in CSkin max and AUC0-8 in compare to rat skin applied with UA-CF gel formulation. Conclusion: The successful optimization and characterization of TN of UA using Box-Behnken design and enhanced dermal delivery reflect the novelty of the work. Present research data showed that the developed TN vesicle formulation was found to be effectively useful drug carrier for UA topical delivery.

Keywords: Ursolic acid, Dermal, Confocal laser scanning microscopy, Dermatokinetic, Skin cancer, Transniosomes, Tumors.