title: Polymer-surfactant nanoparticles for sustained release of water-soluble drugs.
abstract: Poor drug encapsulation efficiency and rapid release of the encapsulated drug limit the use of nanoparticles in biomedical applications involving water-soluble drugs. We have developed a novel polymer-surfactant nanoparticle formulation, using the anionic surfactant Aerosol OT (AOT) and polysaccharide polymer alginate, for sustained release of water-soluble drugs. Particle size of nanoparticles, as determined by atomic force microscopy and transmission electron microscopy, was in the range of 40-70 nm. Weakly basic molecules like methylene blue, doxorubicin, rhodamine, verapamil, and clonidine could be encapsulated efficiently in AOT-alginate nanoparticles. In vitro release studies with basic drug molecules indicate that nanoparticles released 60-70% of the encapsulated drug over 4 weeks, with near zero-order release during the first 15 days. Studies with anionic drug molecules demonstrate poorer drug encapsulation efficiency and more rapid drug release than those observed with basic drugs. Further studies investigating the effect of sodium concentration in the release medium and the charge of the drug suggest that calcium-sodium exchange between nanoparticle matrix and release medium and electrostatic interaction between drug and nanoparticle matrix are important determinants of drug release. In conclusion, we have formulated a novel surfactant-polymer drug delivery carrier demonstrating sustained release of water-soluble drugs.
authors.affiliation: Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA.
authors.forename: Mahesh D
authors.initials: MD
authors.lastname: Chavanpatil
authors.forename: Ayman
authors.initials: A
authors.lastname: Khdair
authors.forename: Yogesh
authors.initials: Y
authors.lastname: Patil
authors.forename: Hitesh
authors.initials: H
authors.lastname: Handa
authors.forename: Guangzhao
authors.initials: G
authors.lastname: Mao
authors.forename: Jayanth
authors.initials: J
authors.lastname: Panyam
mesh_terms: D000464:Alginates / Q000737:chemistry*; D002118:Calcium / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004143:Dioctyl Sulfosuccinic Acid / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D007700:Kinetics; D008956:Models, Chemical; D053758:Nanoparticles; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D012964:Sodium / Q000737:chemistry; D012995:Solubility; D055672:Static Electricity; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D014867:Water / Q000737:chemistry*
chemical_list: D000464:Alginates; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D004364:Pharmaceutical Preparations; D011108:Polymers; D013501:Surface-Active Agents; D014867:Water; D004143:Dioctyl Sulfosuccinic Acid; D020723:Glucuronic Acid; D012964:Sodium; D002118:Calcium