Drug microencapsulation by PLA/PLGA coacervation in the light of thermodynamics. 1. Overview and theoretical considerations.
Phase separation of poly(lactide) (PLA) and poly(lactide-co-glycolide) (PLGA), often called "coacervation" in the pharmaceutical field, is one of the classical methods for peptide drug microencapsulation in biodegradable polyesters. Although numerous studies have used this technique, the underlying physicochemical mechanisms of polyester coacervation under conditions of microsphere production have not been well-described yet. Moreover, the quality of microencapsulation in terms of drug loading efficiency and residual organic solvents is often not entirely satisfactory and depends greatly on the specific drug and polymer used. The first part of this contribution reviews briefly the scientific and patent literature on PLA/PLGA coacervation. Then, the underlying physicochemical principles of polyester coacervation are discussed and relevant thermodynamic models presented. More specifically, attempts were made to clarify the necessary characteristics of polymers, solvents, and coacervating and hardening agents for successful phase separation and microsphere formation. These basic considerations may contribute to a better understanding of the boundary conditions crucial for efficient drug microencapsulation by polyester coacervation.
Thomasin
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The Department of Pharmacy, ETH, Zurich, Switzerland.
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Merkle
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Gander
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D004339:Drug Compounding; D019344:Lactic Acid / Q000737:chemistry*; D008956:Models, Chemical; D011091:Polyesters / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry*; D013816:Thermodynamics
D011091:Polyesters; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C033616:poly(lactide)