Effect of synthetic peptide thrombin receptor agonist encapsulated in microparticles based on lactic and glycolic acid copolymer on healing of experimental skin wounds in mice.
PAR1 peptide thrombin receptor agonist (PAR1-AP) was encapsulated in microcorpuscles based on lactic and glycolic acid copolymer. The desorption profile of the preparation was studied in vitro and its wound-healing effects were studied on a model of cut skin wound in mice. The study showed that 90% PAR1-AP was desorbed over 6 h, but the peptide was detected in eluates from the microparticle surface after 23 h. The desorbed peptide retained its physiological activity and was capable of activating PAR1 receptors on human platelets. The study of the dynamics of experimental skin wound healing in mice showed lower number of macrophages in the wounds treated with PAR1-AP microparticles compared to the control (open wounds and wounds covered with microparticles) and higher number of fibroblasts on day 3 of tissue reparation. Hence, PAR1-AP desorbed from microparticles shortened the inflammation phase in the wound. On day 7 the best healing parameters were also observed in wounds treated with PAR1-AP microparticles, which attests to shortening of the proliferation phase and acceleration of wound healing.
Dugina
T N
TN
Biological Faculty, M. V. Lomonosov Moscow State University, Moscow, Russia. tdugina@mail.ru
Kiseleva
E V
EV
Lange
M A
MA
Vasil'eva
T V
TV
Grandfils
C
C
Markvicheva
E A
EA
Bespalova
Zh D
ZhD
Pal'keeva
M E
ME
Strukova
S M
SM
D000818:Animals; D004337:Drug Carriers; D005260:Female; D005347:Fibroblasts / Q000187:drug effects / Q000502:physiology; D007700:Kinetics; D019344:Lactic Acid; D008264:Macrophages / Q000187:drug effects / Q000502:physiology; D051379:Mice; D010446:Peptide Fragments / Q000627:therapeutic use*; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers; D044463:Receptor, PAR-1 / Q000819:agonists*; D012867:Skin / Q000187:drug effects* / Q000293:injuries / Q000503:physiopathology*; D014945:Wound Healing / Q000502:physiology*
D004337:Drug Carriers; D010446:Peptide Fragments; D011108:Polymers; D044463:Receptor, PAR-1; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid