Abstract
We prepared apigenin (APG)-loaded bilosomes (BLs) and evaluated them for vesicle size, zeta-potential and encapsulation efficiency. The formulations were prepared with cholesterol (CHL), sodium deoxy cholate (SDC), Tween 80 (T80) and phosphatidylcholine (PC) using solvent evaporation method. The prepared formulations showed the optimum result was coated with much mucoadhesive polymer chitosan (CH, 0.25 and 0.5% w/v). The chitosan-coated bilosomes (CH-BLs) were further evaluated for surface morphology, drug–polymer interaction, mucoadhesion, permeation, antimicrobial activity and cell viability. The prepared APG-BLs showed nano-metric size (211 ± 2.87 nm to 433 ± 1.98 nm), polydispersibility index <0.5, negative zeta potential (−15 to −29 mV) and enhanced encapsulation efficiency (69.5 ± 0.93 to 81.9 ± 1.3%). Based on these findings, selected formulation (F2) was further coated with chitosan and showed a marked increase in vesicle size (298 ± 3.56 nm), a positive zeta potential (+17 mV), superior encapsulation efficiency (88.1 ± 1.48%) and improved drug release (69.37 ± 1.34%). Formulation F2C1 showed significantly enhanced permeation and mucoadhesion (p < 0.05) compared to formulation F2 due to the presence of CH as a mucoadhesive polymer. The presence of CH on the surfaces of BLs helps to open the tight membrane junctions and leads to enhanced permeation. A TEM study revealed non-aggregated smooth surface vesicles. The antimicrobial and cell viability assessment revealed better effects in terms of zone of inhibition and cell line assessment against two different cancer cell line. From the study, it can be concluded that APG-CHBLs could be a superior alternative to conventional delivery systems.
Highlights
Apigenin is a flavonoid obtained from fruits, vegetables, and sprouts
The prepared ethosomes were evaluated with tweaks to various parameters, and the results revealed enhanced encapsulation efficiency, skin deposition and transdermal flux
The bacterial cultures were grown in nutrient broth, and each strain was grown to an optical density (OD) of 600 with a bacterial load equivalent of 5 × 106 CFU/mL
Summary
Apigenin is a flavonoid obtained from fruits, vegetables, and sprouts. The therapeutic efficacy of the APG is restricted due to its low water solubility, quick metabolism and low bioavailability. APG-loaded phytosomes have been prepared and optimized using full factorial design [2] They had enhanced solubility, dissolution and in vivo activity. APG-loaded nanoparticles were prepared via anti-solvent precipitation method to enhance solubility and bioavailability [4]. Another research group prepared APG-loaded liposomes via lipid film hydration and evaluated their effect in colorectal cancer [6]. Numerous studies have described use of lipid-based nanoformulations to enhance solubility and dissolution These delivery systems have advantage of a higher effective surface area for drug absorption. Various lipid-based nano-vesicles formulations, such as liposome, niosome, ethosomes, transferosomes and bilosomes [7], have been reported to provide enhanced therapeutic efficacy to poorly water-soluble drugs via different routes.
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