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. 2016 Winter;15(1):83-94.

Development of pH Sensitive Nanoparticles for Intestinal Drug Delivery Using Chemically Modified Guar Gum Co-Polymer

Vegesna Naga Sravan Kumar Varma  1 , Hosakote Gurumalappa Shivakumar  1 , Veerna Balamuralidhara  1 , Manne Navya  1 , Umme Hani  1
Affiliations

Development of pH Sensitive Nanoparticles for Intestinal Drug Delivery Using Chemically Modified Guar Gum Co-Polymer

Vegesna Naga Sravan Kumar Varma et al. Iran J Pharm Res. 2016 Winter.

Abstract

The aim of the research work was to chemically modify guargum (GG) as a pH sensitive co-polymer and formulating intestinal targeting ESO nanoparticles (NPs) using the synthesized co-polymer. Poly acrylamide-grafted-guar gum (PAAm-g-GG) co-polymer was synthesized by free radical polymerization. Chemical modification of PAAm-g-GG by alkaline hydrolysis results in formation of a pH-sensitive co-polymer. The effect of GG and acryl amide (AAm) on grafting was studied. Esomeprazole magnesium (ESO) loaded pH sensitive NPs were prepared by nano-emulsification polymer crosslinking method and characterized. Sixteen formulations were prepared and the concentration of process variables wasvaried to obtain nanoparticles of 200-600 nm. The NPs were found to be homogenous in size distribution. The encapsulation efficiency and drug loading ranged from 33.2% to 50.1% and 12.2% to 17.2% respectively. Particle size, encapsulation efficiency and drug loading increasedalong with co-polymer concentration. In-vitro release studies at pH 1.2 for 2 h, followed by pH 6.8 showed that environment pH significantly affected the drug release. SEM has shown that NPsare spherical with smooth surface. The pH sensitive PAAm-g-GGNPs resisted the initial release of the drug from the drug loaded NPs in acidic pH and delayed the release process to a longer period in alkaline environment.

Keywords: Esomeprazole; PAAm-g-GG; guar gum; intestinal drug delivery; pH sensitive nanoparticles.

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Figures

Figure 1
Figure 1
FT-IR spectra of GG (A), PAAm-g-GG (B) and hydrolyzed PAAm-g GG (C).
Figure 2
Figure 2
Schematic representation of Graft polymerization of acryl amide on guar gum
Figure 3
Figure 3
Schematic representation of Crosslinking of PAAm-g-GG copolymer with glutaraldehyde.
Figure 4
Figure 4
FT-IR spectra of GG (A), PAAm-g-GG (B) and hydrolyzed PAAm-g GG(C
Figure 5
Figure 5
DSC of ESO (A) and F8 (B).
Figure 6
Figure 6
In-vitro drug release profile of various formulations
Figure 7
Figure 7
SEM image of F8
See this image and copyright information in PMC

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