QBD approach for the development of hesperetin loaded colloidal nanosponges for sustained delivery: In-vitro, ex-vivo, and in-vivo assessment
Hesperetin (HT) is a polyphenolic compound with anti-carcinogenic, tumor necrosis, and anti-oxidant properties. The present study reports the fabrication, optimization, and evaluation of HT-loaded nanosponges (HTN)- based gel (HTNG) for sustained anti-inflammatory effect. HTN formulation was prepared by quasi emulsion solvent diffusion method using a 42 factorial design. HTN was subjected to different solid and liquid state characterizations and subsequently loaded in carbopol gel. The effects of pro-inflammatory cytokines (IL- 1β and IL-6) were evaluated using RAW 264.7 macrophage cells, and the anti-inflammatory potential was tested in rats.
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Highlights
• Hesperetin nanosponges were prepared using Quasi emulsion solvent diffusion method.
• Nanosponges were observed to be uniform, mostly spherical, and highly porous.
• Nanosponge based gel profoundly inhibited pro-inflammatory cytokines.
• Nanospones and nanosponge based gel significantly retarded the drug release up to 10 h.
• Nanosponge based gel demonstrated a superior anti-inflammatory effect than neat hesperetin in rats.
Tiny, porous, and spherical HTN retarded the drug release (39.98%) up to 8 h compared to the pure drug (70.74%) and physical mixture (73.72%) and followed the Higuchi-matrix model. HTNG had a strong downregulating effect on cytokines. It showed no skin irritation and 18.52% skin permeation at 8 h. Further, HTNG-treated rats exhibited 33.16% inflammation inhibition compared to the control group. In conclusion, nanosponges significantly retarded the topical delivery and could circumvent the bioavailability issues associated with HT.
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Materials
Hesperetin drug was purchased from Otto, Chemika, Biochemika Reagents, Mumbai, India. Ethylcellulose was procured from High Purity Laboratory Chemicals, Mumbai. Polyvinyl alcohol (PVA), Carbopol 934P, and dichloromethane (DCM) were procured from SD Fine-Chemicals Limited, Mumbai, India. All other chemicals and solvents used were of analytical grade. Double distilled water was used throughout the experimentation.
Kitty Rodrigues, Sameer Nadaf, Nilesh Rarokar, Nilambari Gurav, Pradnya Jagtap, Prashant Mali, Muniappan Ayyanar, Mohan Kalaskar, Shailendra Gurav,
QBD approach for the development of hesperetin loaded colloidal nanosponges for sustained delivery: In-vitro, ex-vivo, and in-vivo assessment, OpenNano, Volume 7, 2022, 100045, ISSN 2352-9520,
https://doi.org/10.1016/j.onano.2022.100045.