Skip to Content
Merck
  • Influence of different formulations and process parameters during the preparation of drug-loaded PLGA microspheres evaluated by multivariate data analysis.

Influence of different formulations and process parameters during the preparation of drug-loaded PLGA microspheres evaluated by multivariate data analysis.

Acta pharmaceutica (Zagreb, Croatia) (2014-12-23)
Jakub Vysloužil, Petr Doležel, Martina Kejdušová, Eliška Mašková, Josef Mašek, Robert Lukáč, Vratislav Košťál, David Vetchý, Kateřina Dvořáčková
ABSTRACT

The main objective of this study was to evaluate the influence of the formulation and process parameters on PLGA microparticles containing a practically insoluble model drug (ibuprofen) prepared by the o/w solvent evaporation method. Multivariate data analysis was used. The effects of altered stirring speed of a mechanical stirrer (600, 1000 rpm), emulsifier concentrations (PVA concentration 0.1 %, 1 %) and solvent selection (dichloromethane, ethyl acetate) on microparticle characteristics (encapsulation efficiency, drug loading, burst effect) were observed. It was found that with increased stirring speed, the PVA concentration or the use of ethyl acetate had a significantly negative effect on encapsulation efficiency. In addition, ethyl acetate had an adverse effect on the burst effect, while increased stirring speed had the opposite effect. Drug load was not affected by any particular variable, but rather by the interactions of evaluated variables.

MATERIALS
Product Number
Brand
Product Description

Supelco
Ibuprofen
Supelco
Phosphate Standard for IC, TraceCERT®, 1000 mg/L phosphate in water (nominal concentration)
Supelco
Ibuprofen, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Sodium phosphate dibasic solution, BioUltra, 0.5 M in H2O
Ibuprofen for peak identification, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Ibuprofen, meets USP testing specifications
Ibuprofen, European Pharmacopoeia (EP) Reference Standard
USP
Ibuprofen, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Ibuprofen, ≥98% (GC)
Sigma-Aldrich
Sodium phosphate dibasic, SAJ first grade, ≥99.0%
Sigma-Aldrich
Sodium phosphate dibasic, ≥99.5%
Sigma-Aldrich
Potassium phosphate monobasic, SAJ first grade, ≥99.0%
Sigma-Aldrich
Dichloromethane, JIS special grade, ≥99.0%
Sigma-Aldrich
Sodium phosphate dibasic, JIS special grade, ≥99.0%
Sigma-Aldrich
Potassium phosphate monobasic, JIS special grade, ≥99.0%
Sigma-Aldrich
Potassium phosphate monobasic, ≥99.5%
Sigma-Aldrich
Dichloromethane, SAJ first grade, ≥99.0%
Supelco
Dichloromethane solution, contains 10 % (v/v) methanol
Sigma-Aldrich
Dichloromethane, HPLC grade
Sigma-Aldrich
Sodium phosphate dibasic, 99.95% trace metals basis
Sigma-Aldrich
Dichloromethane, JIS 5000, for residue analysis
Sigma-Aldrich
Dichloromethane, JIS 300, for residue analysis
Sigma-Aldrich
Potassium phosphate monobasic, 99.99% trace metals basis
Sigma-Aldrich
Dichloromethane, anhydrous, ≥99.8%, contains 40-150 ppm amylene as stabilizer
Supelco
Dichloromethane, Selectophore, ≥99.5%
Sigma-Aldrich
Sodium phosphate dibasic, purum p.a., anhydrous, ≥98.0% (T)
Sigma-Aldrich
Sodium phosphate dibasic, BioUltra, for molecular biology, ≥99.5% (T)
Supelco
Dichloromethane, analytical standard
Sigma-Aldrich
Potassium phosphate monobasic, BioUltra, for molecular biology, anhydrous, ≥99.5% (T)
Sigma-Aldrich
Dichloromethane, suitable for HPLC, ≥99.9%, contains 40-150 ppm amylene as stabilizer