Čes. slov. farm. 2013, 62(3):120-126
Influence of formulation and process parameters on the characteristics of PLGA-based microparticles with controlled drug release
- University of Veterinary and Pharmaceutical Sciences, Department of Pharmaceutics, Faculty of Pharmacy, Brno
PLGA microparticles for sustained release of ibuprofen as the model drug were prepared by the O/W solvent evaporation method under altering stirring speed (600, 1000 rpm), emulsifier concentration (PVA concentration 0.1%, 1%) and organic solvent selection (dichloromethane, ethyl acetate). The obtained results confirmed the effect of selected formulation and process parameters on the properties of prepared PLGA-based microparticles. An influence on encapsulation efficiency, yield, morphological properties, mean size and drug release was observed. Increased stirring speed within the solvent evaporation process resulted in a decrease of encapsulation efficiency, yield and mean size but the incorporated drug was released faster. Increased PVA concentration in the external emulsion phase brought the same results except the ibuprofen release rate. Microparticles prepared with dichloromethane as the organic solvent exhibited higher sphericity, a more regular shape with a smooth surface, and thus dichloromethane was considered to be a more suitable organic solvent in comparison with ethyl acetate for this purpose.
Keywords: microparticles; solvent evaporation; PLGA; controlled release; burst effect
Received: February 22, 2013; Accepted: April 4, 2013; Published: March 1, 2013 Show citation
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References
- Krejčová K., Gryczová E., Rabišková M. Polymeric Microparticles for Oral Administration of Diclofenac Sodium. Chem. Listy 2009; 103, 81-87.
- Li M., Rouaud O., Poncelet D. Microencapsulation by solvent evaporation: State of the art for process engineering approaches. Int. J. Pharm. 2008; 363, 26-39.
Go to original source...
Go to PubMed...
- Pérez M. H., Zinutti C., Lamprecht A., Ubrich N., Astier A., Hoffman M., Bodmeier R., Maincent P. The preparations and evaluation of poly(epsilon;ε-caprolactone) microparticles containing both a lipophilic and a hydrophilic drug. J. Control. Release 2000; 65, 429-438.
Go to original source...
Go to PubMed...
- Rosca I. D., Watari F., Uo M. Microparticle formation and its mechanism in single and double emulsion solvent evaporation. J. Control. Release 2004; 99, 271-280.
Go to original source...
Go to PubMed...
- Giri T. K., Choudhary Ch., Ajazuddin A., Badwaik H., Tripathi D. K. Prospects of pharmaceuticals and biopharmaceuticals loaded microparticles prepared by double emulsion technique for controlled delivery. Saudi Pharm. 2013; 21, 125-141.
Go to original source...
Go to PubMed...
- Tunçay M., Çaliş S., Kaşş H. S., Ercan M. T., Peksoy İ., Hincal A. A. Diclofenac sodium incorporated PLGA (50:50) microspheres: formulation considerations and in vitro/in vivo evaluation. Int. J. Pharm. 2000; 195, 179-188.
Go to original source...
Go to PubMed...
- Klose D., Siepmann F., Elkharraz K., Krenzlin S., Siepmann J. How porosity and size affect the drug release mechanism from PLGA-based microparticles. Int. J. Pharm. 2006; 314, 198-206.
Go to original source...
Go to PubMed...
- Paskaris G., Bouropoulos N. Swelling studies and in vitro release of verapamil from calcium alginate and calcium alginate-chitosan beads. Int. J. Pharm. 2006; 323, 34-42.
Go to original source...
Go to PubMed...
- Wang S. B., Chen A. Z., Weng L. J., Chen M. Y., Xie X. L. Effect of drug-loading methods on drug load, encapsulation efficiency and release properties of alginate/poly-L-arginine/chitosan ternary complex microcapsules. Macromolecular Bioscience 2004; 4, 27-30.
Go to original source...
Go to PubMed...
- Sansdrap P., Moes A. J. Influence of manufacturing parameters on the size characteristics and the release profiles of nifedipine from poly (DL-lactide-co-glycolide) microspheres. Int. J. Pharm. 1993; 98, 157-164.
Go to original source...
- Yang Y. Y., Chung T., Ng N. P. Morphology, drug distribution and in vitro release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. Biomaterials 2001; 22, 231-241.
Go to original source...
Go to PubMed...
- Mainardes R. M., Evangelista R. C. PLGA nanoparticles containing praziquantel: effect of formulation variables on size distribution. Int. J. Pharm. 2005; 290, 137-144.
Go to original source...
Go to PubMed...
- O'Donnell P. B., McGinity J. W. Preparation of microspheres by the solvent evaporation technique. Adv. Drug Delivery Rev. 1997; 28, 25-42.
Go to original source...
Go to PubMed...
- Wang C., Ye W., Zheng Y., Liu X., Tong Z. Fabrication of drug-loaded biodegradable microcapsules for controlled release by combination of solvent evaporation and layer-by-layer self-assembly. Int. J. Pharm. 2007; 338, 165-173.
Go to original source...
Go to PubMed...
- El Bahri Z., Taverdet J. L. Elaboration and characterisation of microparticles loaded by pesticide model. Powder technol. 2007; 172, 30-40.
Go to original source...
- Mao S., Xu J., Cai C., Germershaus O.,Schaper A., Kissel T. Effect of WOW process parameters on morphology and burst release of FITC-dextran loaded PLGA microspheres. Int. J. Pharm. 2007; 334, 137-148.
Go to original source...
Go to PubMed...
- Capan Y., Woo B. H., Gebrekidan S., Ahmed S., DeLuca P. P. Influence of formulation parameters on the characteristics of poly(D, L-lactide-co-glycolide) microspheres containing poly(L-lysine) complexed plasmid DNA. J. Control. Release 1999; 60, 279-286.
Go to original source...
Go to PubMed...
- Mao S., Shi Y., Li L., Xu J., Schaper A., Kissel T. Effects of process and formulation parameters on characteristics and internal morphology of poly(D, L-lactide-co-glycolide) microspheres formed by the solvent evaporation method. Eur. J. Pharm. Biopharmaceutics 2008; 68, 214-223.
Go to original source...
Go to PubMed...
- Fredenberg S., Wahlgren M., Reslow M., Axelsson A.: The mechanisms of drug release in poly(lactic-co-glycolic acid)-based drug delivery systems - a review. Int. J. Pharm. 2011; 415, 34-52.
Go to original source...
Go to PubMed...
- Berchane N. S., Carson K. H., Rice-Ficht A. C., Andrews M. J. Effect of meandiameter and polydispersity of PLGmicrospheres on drug release: Experiment and theory. Int. J. Pharm. 2007; 337, 118-126.
Go to original source...
Go to PubMed...
- Berkland C., Kim K. and Pack D. W. PLG Microsphere Size Controls Drug Release Rate Through Several Competing Factors. Pharmaceut. Res 2003; 20, 1055-1062.
Go to original source...
Go to PubMed...
- Sah. H. Microencapsulation techniques using ethyl acetate as a dispersed solvent: effects of its extraction rate on the characteristics of PLGA microspheres. J. Control. Release 1997; 47, 233-245.
Go to original source...