Nano-delivery of secondary-lipophilic drug system: In vitro | 50129
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International Research Journal of Pharmacy and Pharmacology

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Nano-delivery of secondary-lipophilic drug system: In vitro and ex vivo studies


Susbin Raj Wagle

Probucol is a highly lipophilic drug that has potent anti-inflammatory and anti-oxidant properties. It has been shown to a protective effect on pancreatic β cells and made a potential therapeutic agent in the treatment of T2D. Despite its high efficacy and strong antioxidants effects, PB showed significant variation after oral absorption, poor oral bioavailability, and potentially severe side effects, which restricted its use. This study aimed to examine PB and LCA microcapsules in terms of the microcapsules’ morphology, micro encapsules membrane strength, release kinetics and biological effects ex vivo. Micro encapsules (PB-SA and PB-LCA-SA) were prepared with a Buchi-based microencapsulating system, based on the jet-flow microencapsulation technique using polymer sodium alginate (SA) and examined in vitro (formulation studies) and ex vivo.

Both control and test micro encapsules showed good and uniform morphology characteristics. Incorporation of LCA did not alter the drug content, production yield microencapsulation efficiency, zeta potential, and particle size. However, LCA reduced conductivity, micro encapsules swelling, improved membrane resistance and controlled and targeted release of PB. The micro encapsules swelling and drug release pattern were higher at high pH values (pH 7.8, p<0.05). LCA micro Encapsules enhanced cell viability but not statistically significant, reduced the inflammatory profile (p <0.01), increased anti-inflammatory cytokine and improved bioenergetics parameter (p <0.01). LCA improved the characteristics and release pattern of PB micro encapsules and also enhanced their pharmacological activity in vitro and ex vivo, suggesting potential oral targeted delivery and applications in diabetes treatment.

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