The objectives of this research were to prepare ribavirin niosomes and evaluate the influence of niosomal encapsulation on drug liver targeting in rats. Ribavirin niosomes were prepared by the thin film hydration method using span 60, cholesterol, and dicetyl phosphate in molar ratios of (1:1:0), (4:2:0), (1:1:0.1), and (4:2:1). The prepared niosomes were characterized in vitro for vesicle size, drug entrapment, drug release profiles, and vesicular stability at refrigerator temperature. The results indicated that niosomes of the molar ratio (4:2:1) had a significantly (p < 0.05) higher entrapment percentage of ribavirin than the other molar ratios, moreover, they revealed sustained release characteristics as well as longer release pattern than other niosomal formulations. Accordingly, niosomes of molar ratio (4:2:1) was selected for in vivo liver targeting study. Separately, niosomal ribavirin dispersion and free ribavirin solution were administered as a single dose of 30 mg/kg by intraperitoneal injection into two groups of rats to compare the liver ribavirin concentration. The obtained results show that the niosomal formulation significantly increased ribavirin liver concentration (6-fold) in comparison with ribavirin-free solution. Based on the previous results, the use of niosomes as a drug delivery system for ribavirin has significant liver targeting properties, this is expected to improve the efficacy of low doses of ribavirin and minimize its toxic side-effects at higher doses.
Background:Curcumin is an important natural compound that has been extensively studied for its multifunctional pharmacological activities. Different nanotechnological techniques have been applied for improving its poor solubility and bioavailability. Objectives: This research aimed to study the effect of formulation variables on the entrapment efficiency of curcumin-loaded niosomes (curcusomes) made by a thin-film hydration technique. Methods: Curcumin-loaded noisome were prepared using the thin-film hydration technique using Span 40 and 60 as surfactants, in addition to bile salts and cholesterol. The surfactant and cholesterol were added to curcumin in different ratios, with/without the addition of 10% of bile salts. Results: Eighteen formulae were obtained from the addition of bile salts and spans. Results showed that increased surfactant concentration and low cholesterol ratio enhanced the %EE of formulae. Conclusion: The formulation of curcumin-loaded niosomes with the thin-film hydration method where span 40 or span 60 are used as surfactant enhances the %EE of curcusomes which in turn improves the poor solubility and bioavailability of curcumin. The addition of bile salts enhanced the %EE which will be investigated furtherly for more in vitro and in vivo studies.
Objective: The objective of the present study is to examine the serum stability of siRNA loaded nanoparticles that were prepared with certain polymer and evaluate the influence of different pH values on the in vitro release of siRNA from these particles. Methods: Serum stability of siRNA loaded nanoparticles was studied by incubation in serum free medium and in presence of 10 %, and 25 % serum at 37ºC for 6 h. The unshielded fraction (liable to nucleases) of siRNA was measured by Fluoroskan microplate reader at ex = 485 nm, and em = 518 nm using fluorescence PicoGreen dye. The in vitro release of siRNA from nanoparticles, measured by electrophoresis, was studied in DMEM at two different pH values of 3.5 and 7.4. Results: The results of serum stability showed that 8.6 %, 24.4 %, and 23.5 % siRNA was unshielded from the nanoparticles in the presence of 0 %, 10 %, and 25 % serum, respectively. After 12 h, the released fraction of siRNA was 17.8 % and 95.2 % at pH 7.4 and pH 3.5, respectively. Conclusion: The obtained results revealed that the nanoparticles were considered as a reasonable delivery system that could protect siRNA from degradation by nucleases enzymes upon systemic injection and able to release the loaded siRNA in the acidic pH inside the required cells.
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