Encapsulation and release characteristics of DCTN/PLGA microspheres.
In the present study, poly (D,L-lactic-co-glycolic)-acid microspheres containing trans-Dehydrocrotonin (DCTN) were prepared by the double emulsion method. The hypoglycemic activity of DCTN-loaded microspheres was monitored in normal glycemic mice after administration of a daily dose of DCTN (50 mg kg(-1) body weight) for 7 days. Spherical microspheres with two populations of particles with 3.20 +/- 0.10 and 7.60 +/- 0.70 microm mean diameter size microm were observed. The encapsulation efficiency of DCTN was 85.5 +/- 3.9%. The in vitro kinetic profile of DCTN from PLGA-microspheres was initially fast (burst effect of 19.4% at 2 h). Such a burst step was maintained until achieving 35.7+/-2.0% at 7h, followed by a gradual release of DCTN attaining a maximum drug release at 55.7 +/- 2.6% within 30 h. DCTN was able to reduce glucose levels (14.3%) of normal glycemic animals and this effect was improved by its encapsulation into microspheres (26.8%). The optimum glucose levels in the blood of animals treated with DCTN suspension and DCTN-loaded microspheres were 119.21 +/- 19.75 mg dL(-1) at day 5 and 103.08 +/- 18.88 mg dL(-1) at day 7, respectively. DCTN-loaded microspheres are thus offered as a potential delivery system for the treatment of metabolic diseases characterized by hyperglycemia.
Universidade Federal de Pernambuco (UFPE), Laboratório de Imunopatologia Keizo-Asami (LIKA), Recife, PE, Brazil.
Waldenice A
WA
Morais
Marcilia P
MP
Costa
Ana Durce O
AD
Paixão
Maria Aparecida M
MA
Maciel
Nereide S
NS
Santos-Magalhães
D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D045785:Diterpenes, Clerodane / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004339:Drug Compounding; D005260:Female; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D019344:Lactic Acid / Q000737:chemistry; D051379:Mice; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
D001786:Blood Glucose; D045785:Diterpenes, Clerodane; D007004:Hypoglycemic Agents; C103060:dehydrocrotonin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid