Rutin is a highly potent molecule due to its strong antioxidant properties. In the near future, enhancing its bioavailability using novel drug delivery methods having minimum side effects will bring this promising natural molecule to the forefront of therapy for the treatment of various chronic human diseases.
Iron(ii) bipyridine grafted on graphitic carbon nitride (Fe(bpy)3/npg-C3N4) was found to be an efficient photocatalyst for oxidative coupling of benzyl amines using molecular oxygen as an oxidant and a household white LED as a light emitting source.
The purpose of this study was to investigate the effectiveness and mechanism(s) of percutaneous absorption of propranolol hydrochloride (PHCL) across rat and human cadaver skin using seven novel terpenes with reference to marker terpene 1,8-cineole. In-vitro skin permeation studies were carried out via rat and human skin models. The mechanism of skin permeation of PHCL by terpenes was evaluated by FTIR, DSC, activation energy measurement and histopathological examination. Amongst the new terpenes, 1,4-cineole was found to be most effective enhancer for diffusion of PHCL through rat skin (ER=3.07) and human cadaver skin (ER=2.42) as compared to control. FTIR spectra and DSC thermogram of skin treated with aforesaid terpenes indicated that permeation occurred due to the disruption of lipid bilayers. No apparent skin irritation (erythema, edema) was observed on treatment of skin with terpenes, the irritation was higher with the β-citronellene and rose oxide. It was concluded that 1,4-cineole can be successfully used as potential permeation enhancer for PHCL. It enhanced the absorption of hydrophilic drug by extraction and disruption of lipid bilayers and keratin denaturation of stratum corneum.
Pioglitazone (PZ) an anti-hyperglycemic agent is used in the treatment of type 2 diabetes. The aim of this study was to design PZ-loaded nanostructured lipid carriers (NLC) to investigate the bioavailability improvement by transdermal delivery. PZ NLCs were prepared using highpressure homogenization followed by ultrasonication. The NLCs were evaluated for particle size analysis, drug loading, ex vivo skin transport studies and in vivo bioactivity study. The prepared NLCs had a mean size of 166.05 nm and drug loading of 10.41% with flux value of 47.36 mg/cm 2 /h. The entrapment of PZ is 470% in the NLCs with enhancement ratio of 3.2 times. The in vivo pharmacokinetic study showed 2.17 times enhancement in bioavailability study and pharmacodynamics study showed that PZ NLC-based transdermal therapeutic system (PNLG-TTS) lowers blood sugar level in a sustained pattern for a prolonged period of time as compared to Piosys tablet (marketed). The shelf life of the optimized formulation was found to be 1.83 years. These results clearly provide a lead that above NLCs-based TTS is potential controlled release formulation for PZ and could be a promising drug delivery system for the treatment of diabetes.
A rapid, specific, and sensitive ultra-performance liquid chromatographic (UPLC) method for quantitative analysis of sparfloxacin in bulk drug and pharmaceutical formulations has been developed and validated. In this work, a new gradient reversed-phase chromatographic method was developed. The newly developed method is applicable for assay determination of the active pharmaceutical ingredient. The chromatographic separation of sparfloxacin was achieved on a Waters Acquity HSS T-3 column (100 x 2.1 mm, 1.8 microm) within a short runtime of 5 min. The method was validated according to the ICH guidelines with respect to system suitability, linearity, limit of quantitation and detection, precision, accuracy, robustness, and specificity. Forced degradation studies were also performed for sparfloxacin bulk drug samples to demonstrate the stability indicating power of the UPLC method. Comparison of system performance with conventional HPLC was made with respect to analysis time, efficiency, and sensitivity. The developed method was applied for the assay of marketed sparfloxacin formulations like tablets and eye drops.
Insulin remains indispensable in the management of diabetes mellitus since its discovery in 1921. The foreignness of early available porcine and bovine insulin led to the development of human insulin by transpeptidation and biosynthesis in microorganisms. Needle phobia and stress of multiple daily injections led to the investigation and exploitation of all promising routes, ranging from nasal to rectal, by a wide variety of devices and delivery systems. This article describes the development of human insulin, various routes for delivery of insulin (including oral, nasal, buccal, rectal, and pulmonary), and various devices for regulated, safe, and convenient insulin delivery. The article reviews some recent advances in insulin delivery such as the bioresponsive and self-regulated insulin delivery system.
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