Poly(D,L-lactide-co-glycolide)/hydroxyapatite core-shell nanosphere. Part 2: Simultaneous release of a drug and a prodrug (clindamycin and clindamycin phosphate).
The novel concept of a simultaneous, controlled release of a drug and a prodrug with different physico-chemical properties was applied in order to prolong the release period of antibiotics and estimate their high local concentrations, which are the necessary preconditions for the treatment of some chronic infection diseases. For this purpose poly(D,L-lactide-co-glycolide)/hydroxyapatite (PLGA/HAp) core-shell nanostructures were used as the carrier of clindamycin-base, as a drug, and clindamycin-2-phosphate, as a prodrug model. As a result, a two-step release was observed: the controlled release of the more soluble phosphate form and the sustained release of the less-soluble base form of clindamycin, resulting in a high overall concentration of the released drug during the period of 30 days in vitro. The HAp phase within the PLGA core-shells, applied as a drug carrier, delayed the process of the degradation of the polymer; however, the presence of the drug affected the process of degradation and this influence was the dominant factor in the control over the degradation of the polymer phase of PLGA/HAp and the consequent kinetics of the drug release.
Vukomanović
Marija
M
Institute of Technical Sciences of SASA, Knez Mihailova 35/IV, Belgrade 11000, Serbia. marija.vukomanovic@itn.sanu.ac.rs
Skapin
Srečo Davor
SD
Poljanšek
Ida
I
Zagar
Ema
E
Kralj
Bogdan
B
Ignjatović
Nened
N
Uskoković
Dragan
D
D000327:Adsorption; D000900:Anti-Bacterial Agents / Q000008:administration & dosage; D002151:Calorimetry / Q000379:methods; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D002981:Clindamycin / Q000008:administration & dosage* / Q000031:analogs & derivatives*; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D006882:Hydroxyapatites / Q000737:chemistry*; D019344:Lactic Acid / Q000737:chemistry*; D008422:Materials Testing; D008855:Microscopy, Electron, Scanning / Q000379:methods; D054118:Nanospheres; D036103:Nanotechnology / Q000379:methods*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011355:Prodrugs / Q000008:administration & dosage; D013499:Surface Properties; D014465:Ultrasonics
D000900:Anti-Bacterial Agents; D006882:Hydroxyapatites; D011355:Prodrugs; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D002981:Clindamycin; C007084:clindamycin phosphate