Statistical optimization of bile salt deployed nanovesicles as a potential platform for oral delivery of piperine: accentuated antiviral and anti-inflammatory activity in MERS-CoV challenged mice.
Drug Deliv
; 28(1): 1150-1165, 2021 Dec.
Article
in English
| MEDLINE | ID: covidwho-1271847
ABSTRACT
The objective of this paper is to confine piperine, a poor oral bioavailable herbal drug into bile salt based nano vesicles for improving its aqueous solubility, hence, its therapeutic activity. Piperine-loaded bilosomes were fabricated adopting thin film hydration technique according to 32.21 full factorial design to investigate the impact of different formulation variables on the characters of bilosomes entrapment efficiency (EE%), particle size, and % of drug released post 8 h (Q8hr). The selected optimum formula was F2 (enclosing 1% bile salt, brij72 as a surfactant, and ratio of surfactantcholesterol was 91) with desirability value 0.801, exhibiting high EE% (97.2 ± 0.8%) nanosized spherical vesicles (220.2 ± 20.5 nm) and Q8hr (88.2%±5.6). The superiority of the optimized formula (F2) over the drug suspension was revealed via ex vivo permeation study, also pharmacokinetic study denoted to the boosted oral bioavailability of piperine-loaded bilosome compared to piperine suspension. Moreover, antiviral activity and safety margin of F2 was significantly higher than that of the drug suspension. The ability of piperine to interact with the key amino acids in the receptor binding domain 4L3N as indicated by its docking configuration, rationalized its observed activity. Furthermore, F2 significantly reduce oxidant markers, inflammatory cytokines in MERS-CoV-infected mice. Hence, bilosomes can be considered as a carrier of choice for piperine with potential antiviral and anti-inflammatory activities.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Piperidines
/
Bile Acids and Salts
/
Drug Delivery Systems
/
Alkaloids
/
Benzodioxoles
/
Polyunsaturated Alkamides
/
Middle East Respiratory Syndrome Coronavirus
Type of study:
Randomized controlled trials
Topics:
Traditional medicine
Limits:
Animals
Language:
English
Journal:
Drug Deliv
Journal subject:
Pharmacology
/
Drug Therapy
Year:
2021
Document Type:
Article
Affiliation country:
10717544.2021.1934190
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