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

Autor:	Bhagwat DA; Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra, India. Electronic address: drdabhagwat@gmail.com., Swami PA; Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra, India., Nadaf SJ; Sant Gajanan Maharaj College of Pharmacy, Mahagoan, Site: Chinchewadi 416503, Maharashtra, India., Choudhari PB; Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra, India., Kumbar VM; Central Research Laboratory, Maratha Mandal's Nathajirao G. Halgekar Institute of Dental Sciences & Research Centre, Belgavi, 590 010, Karnataka, India., More HN; Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra, India., Killedar SG; Sant Gajanan Maharaj College of Pharmacy, Mahagoan, Site: Chinchewadi 416503, Maharashtra, India., Kawtikwar PS; Sudhakarrao Naik Institute of Pharmacy, Pusad 445 204, Maharashtra, India.
Jazyk:	angličtina
Zdroj:	Journal of pharmaceutical sciences [J Pharm Sci] 2021 Jan; Vol. 110 (1), pp. 280-291. Date of Electronic Publication: 2020 Oct 15.
DOI:	10.1016/j.xphs.2020.10.020
Abstrakt:	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 < 0.001) inhibited the proliferation of HT-29 colorectal cancer cells than capsaicin. Apoptosis assay involving Annexin V/PI staining for S-CAP-3 treated cells demonstrated a significant (P < 0.001) apoptotic rate. Remarkably, 3.6 fold increase in bioavailability was observed after oral administration of capsaicin-SNEDDS than plain capsaicin. (Copyright © 2020 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.)
Databáze:	MEDLINE
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