Abstract
Purpose: To assess the effect of the lactic acid (LA)-to-glycolic acid (GA) molar ratio and polyethylene glycol (PEG) concentration on the formation of poly-lactide co-glycolide acid (PLGA)-PEG-PLGA co-block polymers simultaneously using statistical approach. Methods: A 22 full factorial design with the addition of a point in the center of the design, namely curvature, was applied. Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and nuclear magnetic resonance (NMR) were performed to confirm the formation of the co-block polymer. Simvastatin (SMV), a drug model was incorporated into the nano-polymeric micellar (NpM) of PLGA-PEG-PLGA followed by solubility phase, particle size, zeta potential, and entrapment efficiency characterizations. Results: FTIR, DSC, and NMR successfully confirmed the formation of co-block polymers. Solubility of SMV increased from 2 to 44-folds depending on co-block concentration with entrapment efficiency of 59%-80%. The NpM had size in the range of 206 to 402 nm with negative zeta potential. LA to GA ratio had greater effect on particle size reduction and increasing of co-polymer length. In addition, it had higher contributions on increasing of solubility and entrapment efficiency of SMV than PEG. Conclusion: According to these findings, the LA to GA ratio and PEG concentration gained a great consideration in order to prepare the PLGA-PEG-PLGA co-block which fulfilled the quality target product profile of NpM delivery system.
Highlights
Delivering a guest molecule to a target site is either attractive owing to major challenges and advantages or a new perspective
Simvastatin (SMV), a drug model was incorporated into the nano-polymeric micellar (NpM) of poly-lactide co-glycolide acid (PLGA)-polyethylene glycol (PEG)-PLGA followed by solubility phase, particle size, zeta potential, and entrapment efficiency characterizations
Preparation of PLGA-PEG-PLGA co-block polymer Preparation of PLGA-PEG-PLGA co-block polymer proceeded according to Scheme 1
Summary
Delivering a guest molecule to a target site is either attractive owing to major challenges and advantages or a new perspective. Several hurdles related to either guest molecule characteristics or physiological condition have emerged.[1,2] Drugs have several issues related to physicochemical properties, by which they are affected with respect to the design of the delivery system. An NpM consists of an amphiphilic compound aggregate where it contains a lipophilic compartment in the inner part (core aggregate) and a hydrophilic compartment in the outer part of the polymer structure.[8,9,10] Like a surfactant, it can enhance bioavailability by elevating solubility and enhance permeation by hindering p-gp efflux owing to modifications of the drug surface by encapsulating with a polymer and steric protection.[11,12] It can be modified to increase the lipophilicity of lipophilic groups to alter the transport mechanism.[9,13]
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