Abstract
BackgroundRepaglinide is an efficient anti-diabetic drug which is prescribed widely as multi-dosage oral daily regimens. Due to the low compliance inherent to each multi-dosage regimen, development of prolonged-release formulations could enhance the overall drug efficacy in patient populations.MethodsRepaglinide-loaded solid lipid nanoparticles (SLNs) were developed and characterized in vitro. Various surfactants were used in this study during the nanocarrier preparation procedure and their corresponding effects on some physicochemical properties of SLNs such as size, zeta potential; drug loading parameters and drug release profiles was investigated. Stearic acid and glyceryl mono stearate (GMS) were used as lipid phase and phosphatidylcholin, Tween80, Pluronic F127, poly vinyl alcohol (PVA) and polyvinyl pyrrolidone (PVP) were used as surfactant/stabilizer.ResultsThe results showed some variations between formulations; where the Tween80-based SLNs showed smallest size, the phosphatidylcholin-based SLNs indicated most prolonged drug release time and the highest loading capacity. SEM images of these formulations showed morphological variations and also confirmed the nanoscale size of these particles. The FTIR and DSC results demonstrated no interaction between drug and excipients. The invitro release profiles of different formulations were studied and observed slow release of drug from all formulations. However significant differences were found among them in terms of their initial burst release as well as the whole drug release profile. From fitting these data to various statistical models, the Peppas model was proposed as the best model to describe the statistical indices and, therefore, mechanism of drug release.ConclusionThe results of this study confirmed the effect of surfactant type on SLNs physicochemical properties such as morphological features, loading parameters, particle sizes and drug release kinetic. With respect to the outcome data, the mixture of phosphatidylcholin/Pluronic F127 was selected as the best surfactant/stabilizer to coat the lipid core comprising stearic acid and GMS.
Highlights
Diabetes mellitus is a wide spread chronic disease with serious life-threatening effects on different parts/ functions throughout the body
The results of this study confirmed the effect of surfactant type on SLNs physicochemical properties such as morphological features, loading parameters, particle sizes and drug release kinetic
Preparation of SLNs SLNs were prepared by a modified solvent diffusion method, where ethanolic phase containing 150 mg stearic acid, 50 mg glyceryl mono stearate (GMS) and 50 mg repaglinide was diffused in aqueous phase under magnetic stirring condition (1000 g) at 50 °C with an addition rate of 1 ml/min and, the resulting dispersion was allowed cooling until the room temperature
Summary
Diabetes mellitus is a wide spread chronic disease with serious life-threatening effects on different parts/ functions throughout the body. The majority of diabetic patients are found to be type ІІ diabetes mellitus, i.e., (non-insulin-dependent). To manage this type of diabetes, different classes of oral anti-diabetic drugs are used routinely in the market [1]. Repaglinide causes hypoglycemia following oral administration, the extent of this feature is less than the sulphonylureas [2]. These properties have proposed the drug as a good candidate for sustain oral delivery formulations. Repaglinide is an efficient anti-diabetic drug which is prescribed widely as multi-dosage oral daily regimens. Due to the low compliance inherent to each multi-dosage regimen, development of prolonged-release formulations could enhance the overall drug efficacy in patient populations
Sign-in/Register to view highlights & summary 
Published Version (
Free)
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call