Optimizing nutraceutical-loaded trehalosomes in-situ gel for diabetic cataract management: Comprehensive in vitro and in vivo evaluations

Abstract

This study aimed to develop Baicalin-loaded trehalosomes in situ gel (BA-THs-ISG) for the treatment of cataract, a degenerative eye condition that requires innovative approaches to enhance visual acuity and quality of life. A 33 D-optimal design was implemented for the preparation and statistical optimization of BA-THs. Various in-vitro studies were conducted to evaluate the features of the optimized formula, which was subsequently loaded into an optimum ISG to sustain the release pattern. To assess the therapeutic efficacy of BA-THs-ISG, an in-vivo study was conducted using a streptozotocin (STZ) induced diabetic cataract model. The results demonstrated that the optimized formula of desirability function of 0.878 had a particle size (PS) of 237.9 ± 2.87 nm, a polydispersity index (PDI) of 0.27 ± 0.03, a zeta potential (ZP) of −27.31 ± 1.27 mV, an entrapment efficiency (EE%) of 74.32 ± 1.08 % and sustained drug release over 6 h. After being loaded into ISG, BA-THs-ISG exhibited a gelation temperature of 35.00 ± 0.30 °C and a gelation time of 49 ± 2.63 s, meeting the intended criteria. Moreover, it effectively maintained drug release for a duration of 12 h. Compared to the BA solution in the in-vivo studies, BA-THs-ISG significantly reduced malondialdehyde content and enhanced superoxide dismutase and glutathione peroxidase activities without any irritation potential. Therefore, BA-THs-ISG is inferred to be a highly effective option for improving cataract symptoms.