Thrombin receptor agonist peptide entrapped in poly(D,L)-lactide-co-glycolide microparticles: preparation and characterization.
Thrombin receptor agonist peptide (TRAP-6) could advantageously replace thrombin in terms of accelerating wound healing being less expensive and more stable. To promote TRAP-6 pharmacological action as a tissue reconstruction stimulator this study investigated its entrapment within poly(D,L)-lactide-co-glycolide (PLGA) microparticles. Due to its low molecular weight and water solubility, TRAP-6 microencapsulated form is expected to be more useful. This paper reports TRAP-6 microencapsulation by a double (w/o/w) emulsion-evaporation technique. TRAP-6 release kinetics were evaluated by both chemical (HPLC) and biological assays in vitro. The results revealed a high level of TRAP-6 sensitivity to physico-chemical events during the microencapsulation. The surface morphology difference between control microparticles (without TRAP-6) and microparticles with entrapped TRAP-6 during in vitro degradation highlighted a particular role of TRAP-6. The results can allow one to optimize the microencapsulation procedure and to encounter a new promising approach to development of biodegradable polymer drug delivery systems for wound healing.
Stashevskaya
Kira
K
Russian Academy of Sciences, Polymers for Biology Laboratory, Shemyakin & Ovchinnikov Institute of Bioorganic Chemistry, Moscow, Russia.
Markvicheva
Elena
E
Strukova
Svetlana
S
Prudchenko
Igor
I
Zubov
Vitaly
V
Grandfils
Christian
C
D001792:Blood Platelets / Q000187:drug effects / Q000502:physiology; D002214:Capsules; D003692:Delayed-Action Preparations; D004655:Emulsions; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D010446:Peptide Fragments / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D010455:Peptides / Q000737:chemistry*; D011098:Polyglactin 910; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry; D018179:Receptors, Thrombin / Q000819:agonists*; D014945:Wound Healing / Q000187:drug effects
D002214:Capsules; D003692:Delayed-Action Preparations; D004655:Emulsions; D010446:Peptide Fragments; D010455:Peptides; D011108:Polymers; D018179:Receptors, Thrombin; C082835:thrombin receptor peptide (42-47); D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011098:Polyglactin 910