development characterization and optimization of colon targeted nanoparticulate drug delivery system of anti inflammatory agent

Abstract

The aim of the present research work was the development and characterization of a colon-targeted drug delivery system for quercetin dihydrate (QDH). Quercetin dihydrate (QDH) is a naturally occurring anti-inflammatory agent. The drug was poorly water soluble in nature and was found to have low bioavailability. The prepared nanoparticles were characterized for various evaluation parameters like particle size (PS), polydispersity index (PDI) and cumulative % drug release (% CDR). newlineTo achieve the present aim of research work, initially QDH loaded chitosan nanoparticles (QLCN) were prepared using ionic gelation technique. The prepared QLCN were optimized using rotatable central composite design. The average PS of optimized batch of QLCN was 109.3 ± 2.76 nm, PDI was 0.396 ± 0.02 and % EE was 80.4 ± 1.06. Furthermore, optimized batch of QLCN was subjected to Scanning electron microscopy (SEM) analysis. According to SEM analysis, nanoparticles particles exhibited slightly rough surfaces and were spherical in appearance. There was also no particle aggregation seen in the micrographs. newlineOil-in-oil solvent evaporation process was used for coating of Eudragit S 100 (ES 100) on QLCN to achieve colon targeted QLCN (ES-QLCN). To optimize formulation of ES-QLCN, Box- Behnken Design (BBD) was used. Where Core: Coat ratio (X1), Dispersed phase: Continuous phase ratio (DP: CP ratio) (X2) and Concentration of surfactant (X3) were selected as three independent variables. The dependent variables selected were PS (Y1), PDI (Y2) and %EE (Y3), % CDR) at 2 hrs (Y4) and 12 hrs (Y5). Optimized formulation of ES 100 coated QLCN (ES-QLCN) showed an average PS 234.6 ± 2.48 nm, PDI 0.318 ± 0.01, % EE 73.7 ± 2.06 and % CDR at 2 hrs and 12 hrs were found to be 3.82 ± 0.59 % and 64.83 ± 1.13 % respectively. newlineSEM analysis of ES-QLCN revealed that the nanoparticles had smooth surfaces and were spherical in nature. No particle agglomeration was observed in the micrograph. The DSC thermogram of ES-QLCN showed that the drug might have been dispersed o