Formulation of sitagliptin-loaded oral polymeric nano scaffold: process parameters evaluation and enhanced anti-diabetic performance.
Artif Cells Nanomed Biotechnol. 2017 Dec 09;:1-13
Authors: Jahangir MA, Khan R, Sarim Imam S
Abstract
PURPOSE: The aim of the study to formulate and statistically optimize sitagliptin-loaded eudragit nanoparticles (SIT-NPs) and evaluate the in-vitro pharmaceutical quality and in-vivo anti-diabetic assessment.
METHOD: SIT-NPs were prepared by using combination method of solvent evaporation and nano-precipitation techniques. The influence of different independent variables as eudragit RL100 concentration (%), tween 80 concentration (%) and sonication time (min) were evaluated on dependent variables like particle size (nm), drug loading (%) and in-vitro drug release (%). Further, the optimized formulation was evaluated for surface morphology, CLSM, ex-vivo permeation study and in-vivo anti-diabetic activity and stability study.
RESULTS: The developed SIT-NPs formulations showed particle size range (135.86-193.45 nm), drug loading (6.36-8.76%) and prolonged drug release over 24 h. The prepared SIT-NPs were found to be nearly spherical with smooth surface. The comparative in-vitro release study and CLSM study results revealed that SIT-NPopt showed significantly (p < .05) enhanced release and permeation as compared to SIT free solution (SIT-Fs). The in-vivo anti-diabetic assessment revealed that SIT-NPopt able to reduce the blood sugar level (BSL) for a prolonged period of time. Further, the stability study data showed the formulations were found stable at both temperature and having the shelf life of 488 d.
CONCLUSIONS: This research has shown that SIT-NPs based on experimental design offers a new and better approach to delivering SIT, thus encouraging further development of this formulation.
PMID: 29226729 [PubMed - as supplied by publisher]
http://ift.tt/2l7mdAE
Δεν υπάρχουν σχόλια:
Δημοσίευση σχολίου