<p>In vitro Characterization and Release Studies of Combined Nonionic Surfactant-Based Vesicles for the Prolonged Delivery of an Immunosuppressant Model Drug</p>

Abstract

Background: Cyclosporine A (CsA) is an exceptional immunosuppressant used for the treatment of immune disorders. Niosomal vesicles are promising drug carriers that are formed by self-association of nonionic surfactants and cholesterol in an aqueous phase. The objective of the study was to formulate combined nonionic surfactant based vesicles and to evaluate their in vitro characterization, release studies and in vivo studies. Materials and Methods: Five niosomal formulations (F 7 to F 11) were prepared using the thin film hydration method. The molar ratio of cholesterol and non-ionic surfactant taken was 1:1. In formulation F 10 , the combination of surfactants Span 20 and Brij 35 was used. The niosomes were characterized by zeta sizer and SEM for particle size analysis, in vitro drug release and stability studies. The pharmacokinetic studies were conducted on healthy albino rabbits. Results: The size of niosome was found in the range of 427.1 nm to 972.3 nm. SEM image of optimized formulations F 10 exhibit the spherical nature of niosomal vesicles. DSC thermograms of niosomal formulations exhibited a broadened endothermic peak. The stability study exhibited that all formulations are stable and negligible change of vesicle size and entrapment was observed with time. The percentage drug release was significantly higher as compared to CsA plain dispersion for all niosomal formulations at pH 1.2 and 7.4. The release kinetic behavior showed that all preparations were best described by zero order and can release active ingredient in a sustained manner. The pharmacokinetic data showed the test formulation (F10) possessed greater bioavailability as compared to the reference formulation (CsA aqueous dispersion). Conclusion: The formulation F 10 demonstrated a comparatively more delayed rate of release with enhanced dissolution as compared to a single surfactant scheme. The F 10 formulation can be a remarkable nanotechnology for prolonged delivery of CsA orally with improved dissolution profile and bioavailability.

Statistically-Based Optimization of Verapamil Hydrochloride Loaded Gastroretentive Alginate Beads

“…The behavior of drug release from the prepared formulations followed sustained pattern over 8 hr. The in vitro drug release from (F1, F2, F5, F6, F7 and F8) was best fitted zero order release kinetics indicating that these formulations were able to release equal quantity of VerHCl per unit of time which is the best manner of drug release to achieve a delayed effect 40 .The release data of F3 was fitted to Hixson-Crowell cube root law which describes the dissolution controlled release from systems where there is a change in surface area and diameter of the particles 41 . The formula F4 was most fitted to Higuchi diffusion model where the drug diffuses at a slower rate as the distance for diffusion increases, which is referred as square root time dependent kinetics.…”

Niosomes-loaded selenium nanoparticles as a new approach for enhanced antibacterial, anti-biofilm, and anticancer activities

“…The main composition of the F2 formulation was Span 60, Tween 60 with cholesterol, which is expected to produce a rigid vesicle membrane. Also, several studies showed that the use of Tween 80 in the preparation of niosomes causes their fluidity and the release rate of the vesicular membrane increases 40 . The release characteristics of SeNPs from niosomes potentially meet the requirements of an in-use antimicrobial delivery system.…”

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“…Span 60 and tween 60 were two nonionic surfactants used in niosomal formulation F TS and span 20 and brij 35 were utilized in F SB . The higher lipid concentration, uniform vesicle size and mixed nonionic surfactants results in augmented bioavailability (Rasul et al, 2020). The peak plasma concentration (C max ) is the highest concentration that active pharmaceutical agent accomplishes in the blood circulation after dose administration.…”