The study aims to elaborate novel self-assembled liquid crystalline nanoparticles (LCNPs) of resveratrol which has neuro-protective, anti-aging, and anticancer activity. Resveratrol loaded LCNPs fabrication and optimization for transdermal delivery was assessed via a quality by design approach based on 2 full factorial designs. The cubic phase of LCNPs was successfully prepared using GMO (glyceryl monooleate) via the emulsification technique. Based on the factorial design, the independent operating variables significantly affected the five dependent responses. The cubosomes and hexosomes hydrodynamic diameters were in the nanometer range (135-256 nm) with narrow particle size distribution, high negative zeta potential ≥ -27.9 mV, and entrapment efficiency ≥73.5%. The LCNPs succeeded in sustaining resveratrol release for almost 24 h, following a non-fickian transport of drug diffusion mechanism. Ex-vivo study revealed a significant enhancement up to six folds in the transdermal permeation of resveratrol-loaded LCNPs compared to its suspension. The selected LCNPs exhibited a high physical stability while retaining the cubic structure for at least 3 months. Quality by design approach successfully accomplished a predictable mathematical model permitting the development of novel LCNPs for sustained transdermal delivery of resveratrol.
This study aims at formulating solid lipid nanoparticles (SLNs) of Vinpocetine (VIN) to be used as a brain targeted sustained drug-delivery system. VIN is a derivative of vincamine alkaloid, used for chronic cerebral vascular ischemia. However, it suffers from low bioavailability and short half-life. Its oral bioavailability is recorded to be between 7 and 55%. Its elimination half-life is 1-2 h so it would be a good candidate for a sustained drug-delivery system. VIN SLNs were prepared using modified high shear homogenization followed by ultrasonication technique. The effect of incorporating different lipids at different concentrations of various surfactants was investigated. The VIN SLNs were characterized by entrapment efficiency percent (EE%), particle size distribution, zeta-potential, and cumulative released percent after 96 h. The EE% ranged between 83.34% ± 0.95-94.56% ± 0.11 due to the lipophilic character of VIN. The mean particle size measured ranged from 123 nm-464 nm. The cumulative released percent after 96 h ranged from 23.55% to 75.67% showing a controlled release profile. Formula (F32) composed of 5% glyceryl monostearate (GMS) and stabilized by 2% surfactant mixture [Tween 80, Pluronic F 68 (1:1)] was the most appropriate formula for brain delivery having EE% of 89.09% ± 1.49, zero-order release kinetics with cumulative released percent of 72.12% after 96 h, zeta-potential of -11.3 ± 0.97 mV. It showed a unimodal size distribution with particle size ≈ 90 nm and polydispersity index of 0.121. The formula of choice in this study exhibited a zero-order sustained release profile and met the requirement for a brain targeted SLN so it could be a promising formula to deliver VIN to the brain.
Agomelatine (AGO) is a dual-functional drug. It uses as an antidepressant when orally administrated and antiglaucomic when topically applied to the eye. This study aimed to formulate AGO into bilosomal vesicles for glaucoma treatment, as modern studies pointed out the effect of topical AGO on intraocular pressure for the treatment of glaucoma. A modified ethanol injection technique was used for the fabrication of AGO bilosomes according to a D-optimal design. Phosphatidylcholine (PC) to edge activator (EA) ratio, Hyaluronic acid percentage (HA%), and EA type were utilized as independent variables. The measured responses were percent entrapment efficiency (EE%), particle size (PS), polydispersity index, zeta potential, percentage of drug released after 2 h (Q
2h%
), and 24 h (Q
24h%
). The optimal bilosomal formula (OB), with the desirability of 0.814 and the composition of 2:1 PC: EA ratio, 0.26% w/v HA and sodium cholate as EA, was subjected to further
in vitro
characterizations and
in vivo
evaluation studies. The OB formula had EE% of 81.81 ± 0.23%, PS of 432.45 ± 0.85 nm, Q
2h%
of 42.65 ± 0.52%, and Q
24h%
of 75.14 ± 0.39%. It demonstrated a higher elasticity than their corresponding niosomes with a typical spherical shape of niosomes by using transmission electron microscope. It exhibited acceptable stability over three months. pH and Refractive index measurements together with the histopathological study ensured that the OB formula is safe for the eye and causes no ocular irritation or blurred vision. The OB formula showed superiority in the
in vivo
pharmacodynamics parameters over the AGO solution, so AGO-loaded bilosome could improve ocular delivery and the bioavailability of agomelatine.
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