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

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, microencapsules membrane strength, release kinetics and biological effects ex vivo. Microencapsules (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 microencapsules 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, Microencapsules swelling, improved membrane resistance and controlled and targeted release of PB. The microencapsules swelling and drug release pattern were higher at high pH values (pH 7.8, p<0.05). LCA microencapsules 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 microencapsules and also enhanced their pharmacological activity in vitro and ex vivo, suggesting potential oral targeted delivery and applications in diabetes treatment.

Author(s):  Wagle Susbin

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