Controlled release from bioerodible polymers: effect of drug type and polymer composition.
The effect of the chemical nature of the drug on matrix degradation and drug release behavior of degradable polymers was studied, using lidocaine as a model drug in base and salt forms. We show in this study that the drug in the base form has a substantial effect on the release characteristics, through an accelerating effect on matrix degradation. Study of drug release from PdlLGA shows that lidocaine salt follows a three-phase release pattern, in contrast to the biphasic release of the lidobase. However, PlLA shows a different drug release pattern, with only a single diffusion phase exhibited for both lidobase and lidosalt. We also demonstrate that the crystallinity of matrix plays an important role on drug release profiles: a crystalline matrix (PlLA IV=2.04) releases the drug at a much slower rate compared to its amorphous counterpart of similar molecular weight (PdlLA IV=2.4). The details of the study of different factors influencing the drug release may have important implications for the control of delivery of potent drugs in various therapeutic windows.
Frank
Alexis
A
School of Materials Engineering, N4.1-1-30, Nanyang Technological University, Nanyang Avenue, Singapore 639798, Singapore.
Rath
Santosh Kumar
SK
Venkatraman
Subbu S
SS
D000465:Algorithms; D000779:Anesthetics, Local / Q000008:administration & dosage / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002850:Chromatography, Gel; D003692:Delayed-Action Preparations / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D007700:Kinetics; D019344:Lactic Acid; D008012:Lidocaine / Q000008:administration & dosage / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D008970:Molecular Weight; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D014867:Water / Q000737:chemistry
D000779:Anesthetics, Local; D003692:Delayed-Action Preparations; D005079:Excipients; D011108:Polymers; D014867:Water; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D008012:Lidocaine