Abstract
An initial burst is often observed during the release of active pharmaceutical ingredients (APIs) from poly-lactic-coglycolic-acid (PLGA) microparticles (MPs) which have been prepared by the emulsion-solvent evaporation method. Herein, we describe the development of a simple one-step coating method that suppresses the initial burst release process. This new method involves coating the PLGA-MPs with PLGA, with the coating process being performed through the phase separation of PLGA on the surface of PLGA-MPs using the emulsion-solvent evaporation method. Bovine serum albumin (BSA) was encapsulated in the PLGA-MPs as a model API. The coated MPs were spherical in shape with no pores on their smooth surface, whereas the non-coated PLGA-MPs had porous surfaces. An in vitro release study showed that the residual levels of BSA in the coated and non-coated PLGA-MPs after 1 h were about 99% and 16% of the original loads, respectively. The one-step coating method therefore represents a useful method for preparing PLGA-MPs that do not give an initial burst release of proteinaceous APIs.
Highlights
Biocompatible and biodegradable synthetic polymers such as poly-lactic-co-glycolic-acid (PLGA) have been used as base materials in a number of different functional materials, such as absorbable biomaterial implants [1,2], absorbable surgical sutures [3,4] and microparticles (MPs) for the sustained release of active pharmaceutical ingredients (APIs) including bioactive proteins [5]
The PLGA-MPs had to be dispersed in peanut oil to enable the formation of an oil layer on their surface to prevent the dissolution and aggregation of PLGA-MPs during the PLGA coating, indicating that this coating method still required a series of time-consuming steps
One of the major advantages of PLGA coatings is that the encapsulated APIs can be released from the PLGA-MPs at a constant rate because the degradation rates of PLGA are similar in the MPs and the coating layer
Summary
Biocompatible and biodegradable synthetic polymers such as poly-lactic-co-glycolic-acid (PLGA) have been used as base materials in a number of different functional materials, such as absorbable biomaterial implants [1,2], absorbable surgical sutures [3,4] and microparticles (MPs) for the sustained release of active pharmaceutical ingredients (APIs) including bioactive proteins [5]. Several methods have been developed to suppress the initial burst release of APIs from PLGA-MPs, including the replacement of PLGA with different materials with slower degradation rates [8,9,10],. One-Step Preparation of Poly-Lactic-Co-Glycolic-Acid Microparticles to Prevent the Initial Burst Release of Encapsulated Water-Soluble Proteins method of coating PLGA-MPs with PLGA [17]. We have developed a simple onestep method for coating PLGA-MPs with PLGA during the final step of the emulsion-solvent evaporation method. PLGA-MPs encapsulated with bovine serum albumin (BSA) (BSA-MPs) were coated with PLGA using the current method to evaluate the general utility of this one-step coating method as a means of suppressing the initial burst release of proteinaceous APIs (Figure 1), and their physicochemical properties and protein-release behaviors were investigated
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