The purpose of the current study was to develop tizanidine HCl (TIZ; a myotonolytic agent used for treatment of spasticity) loaded nanotransfersomes intended for rectal administration, aiming to bypass the hepatic first-pass metabolism. TIZ-loaded nanotransfersomes were prepared by thin-film hydration method followed by characterization for various parameters including entrapment efficiency, vesicle diameter, in vitro release and ex vivo permeation studies. Transfersomal formulation composed of phosphatidylcholine and Tween 80 at a weight ratio of (85:15) gave a satisfactory results. It exhibited encapsulation efficiency of 52.39%, mean diameter of 150.33 nm, controlled drug release over 8 h and good permeation characteristics. Optimum formula was then incorporated into Pluronic-based thermoreversible gel using hydroxypropyl methylcellulose (HPMC) as a mucoadhesive polymer. Pharmacokinetic study was performed by rectal administration of transfersomes-loaded in situ gel to rabbits and compared with oral drug solution and rectal TIZ in situ gel. The pharmacokinetic study revealed that the transfersomal formulation successively enhanced the bioavailability of TIZ by about 2.18-fold and increased t 1/2 to about 10 h as compared to oral solution. It can be concluded that encapsulation of TIZ into nanotransfersomes can achieve a dual purpose of prolonged TIZ release and enhanced bioavailability and so may be considered as a promising drug delivery system for the treatment of spasticity.
This study was conducted to investigate the preventive effects of Chitosan-nanoparticles on diethylnitrosamine (DEN) induced hepatotoxicity in albino rats. Forty male albino rats were divided into four groups: group (1): normal control, group (2): group (2): hepatotoxic rats administrated DEN orally (20 mg/kg b.wt/ day), group (3): rats receive chitosan-nanoparticles orally and group (4): Hepatotoxic rats were treated with chitosan-nanoparticles orally at a dose of (200 mg / kg bw/day). All animals were sacrificed at the end of experiment (12 weeks). The hepatotoxic effect of DEN was evidenced by elevation of serum Aspartate Aminotransferase, Alanine Aminotransferase, Alkaline Phosphatase, γ-Glutamyl transferase activities, blood Urea concentration and liver Malondialdehyde level. However serum albumin concentration and antioxidants biomarkers in liver tissue were markedly decreased. In conclusion, the administration of chitosan nanoparticles restored the DEN induced alterations in liver functions, promoted oxidative stress and antioxidant defense
While oral agents have been the gold standard for cardiovascular disease therapy, the new generation of treatments is switching to other administration options that offer reduced dosing frequency and more efficacy. The lymphatic network is a unidirectional and low-pressure vascular system that is responsible for the absorption of interstitial fluids, molecules, and cells from the peripheral tissue, including the skin and the intestines. Targeting the lymphatic route for drug delivery employing traditional or new technologies and drug formulations is exponentially gaining attention in the quest to avoid the hepatic first-pass effect. The present review will give an overview of the current knowledge on the involvement of the lymphatic vessels in drug delivery in the context of cardiovascular disease.
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