Capsaicin Loaded Solid SNEDDS for Enhanced Bioavailability and Anticancer Activity : In-Vitro, In-Silico, and In-Vivo Characterization
Copyright © 2020 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved..
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:110 |
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| Enthalten in: |
Journal of pharmaceutical sciences - 110(2021), 1 vom: 15. Jan., Seite 280-291 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Bhagwat, Durgacharan A [VerfasserIn] |
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| Links: |
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| Themen: |
Annexin V/PI staining |
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| Anmerkungen: |
Date Completed 17.06.2021 Date Revised 17.06.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.xphs.2020.10.020 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM31639145X |
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| 520 | |a Copyright © 2020 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved. | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Annexin V/PI staining | |
| 650 | 4 | |a Apoptosis | |
| 650 | 4 | |a Bioavailability | |
| 650 | 4 | |a Cancer | |
| 650 | 4 | |a Capsicum annuum | |
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| 650 | 7 | |a Capsaicin |2 NLM | |
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| 700 | 1 | |a Swami, Pratik A |e verfasserin |4 aut | |
| 700 | 1 | |a Nadaf, Sameer J |e verfasserin |4 aut | |
| 700 | 1 | |a Choudhari, Prafulla B |e verfasserin |4 aut | |
| 700 | 1 | |a Kumbar, Vijay M |e verfasserin |4 aut | |
| 700 | 1 | |a More, Harinath N |e verfasserin |4 aut | |
| 700 | 1 | |a Killedar, Suresh G |e verfasserin |4 aut | |
| 700 | 1 | |a Kawtikwar, Pravin S |e verfasserin |4 aut | |
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