Capsaicin Loaded Solid SNEDDS for Enhanced Bioavailability and Anticancer Activity: In-Vitro, In-Silico, and In-Vivo Characterization

• Published in: Journal of pharmaceutical sciences 2021-01, Vol.110 (1), p.280-291
• Main Authors: Bhagwat, Durgacharan A., Swami, Pratik A., Nadaf, Sameer J., Choudhari, Prafulla B., Kumbar, Vijay M., More, Harinath N., Killedar, Suresh G., Kawtikwar, Pravin S.
• Format: Article
• Language: English
• Subjects: Annexin V/PI staining; Apoptosis; Bioavailability; Cancer; Capsicum annuum
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1016/j.xphs.2020.10.020

In this investigation, the fabrication of capsaicin loaded self nano emulsifying drug delivery system (SNEDDS) was attempted to improve the effectiveness of capsaicin through the oral route. A pseudo-ternary phase diagram was constructed at different km values (1:1, 2:1, & 3:1). Nine liquid formulations (L–CAP-1 to L–CAP-9) were prepared at km = 3, evaluated & converted to solid free-flowing granules using neusilin® US2. L–CAP-3 comprising of 15% isopropyl myristate, 33.75% Labrafil, & 11.25% ethanol exhibited higher % transmittance (98.90 ± 1.24%) & lower self-emulsification time (18.19 ± 0.46 s). FT-IR spectra showed no incompatibility whereas virtual analysis confirmed hydrogen bond interaction between amino hydrogen in the capsaicin & oxygen of the neusilin. DSC & XRD study revealed the amorphization & molecular dispersion of capsaicin in S-SNEDDS. TEM analysis confirmed the nano-sized spherical globules. Within 15 min, L-SNEDDS, S-SNEDDS, & pure capsaicin showed 87.36 ± 3.25%, 85.19 ± 4.87%, & 16.61 ± 3.64% drug release respectively. S-CAP-3 significantly (P