Novel pH-sensitive polyacetal-based block copolymers for controlled drug delivery

The principal aim of this study was to synthesize and characterize pH-sensitive biodegradable triblock copolymers containing a hydrophobic polyacetal segment for controlled drug delivery. Poly(ethylene glycol)–poly(ethyl glyoxylate)–poly(ethylene glycol) (PEG–PEtG–PEG) triblock copolymers with PEG m...

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Bibliographic Details
Published in:International journal of pharmaceutics 2010-11, Vol.401 (1), p.79-86
Main Authors: Kim, Jin-Ki, Garripelli, Vivek Kumar, Jeong, Ui-Hyeon, Park, Jeong-Sook, Repka, Michael A., Jo, Seongbong
Format: Article
Language:English
Subjects:
Acetals - chemistry
Antineoplastic Agents, Phytogenic - administration & dosage
Antineoplastic Agents, Phytogenic - chemistry
Biodegradable
Biological and medical sciences
Chromatography, Gel
Chromatography, High Pressure Liquid
Controlled release
Drug Delivery Systems
General pharmacology
Hydrogen-Ion Concentration
Magnetic Resonance Spectroscopy
Medical sciences
Micelles
Paclitaxel - administration & dosage
Paclitaxel - chemistry
pH-sensitive
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyacetal
Polyethylene Glycols - chemistry
Polymeric micelles
Polymers - chemistry
Solubility
Temperature
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Summary:The principal aim of this study was to synthesize and characterize pH-sensitive biodegradable triblock copolymers containing a hydrophobic polyacetal segment for controlled drug delivery. Poly(ethylene glycol)–poly(ethyl glyoxylate)–poly(ethylene glycol) (PEG–PEtG–PEG) triblock copolymers with PEG molecular weights 500 (PEtG–PEG 500) and 750 (PEtG–PEG 750) were synthesized by PEtG end-capping with methoxy PEG via a carbamate linkage. Synthesized amphiphilic PEG–PEtG–PEG was characterized by 1H NMR spectroscopy. Molecular weights of PEtG–PEG 500 and PEtG–PEG 750 were determined to be 2823 and 3387, respectively, by gel permeation chromatography. The polymers with a biodegradable polyacetal block underwent pH-dependent degradation via an acid-catalyzed hydrolysis. Paclitaxel (PTX)-loaded polymeric micelles were prepared by a dialysis method and the amount of PTX incorporated into the polymeric micelle formulations was 45,000 times greater than the water solubility of PTX at room temperature. The polymeric micelles prepared from the amphiphilic PEG–PEtG–PEG triblock copolymers have released the loaded PTX in a pH-dependent manner. The novel PEtG-based amphiphilic block copolymers can find applications for targeted and controlled drug delivery to the acidic environments found in tumors and intracellular compartments.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2010.08.029