[Preparation and properties of Talpha1 loaded injectable sustained release microspheres].
To prepare thymosin alpha-1 (Talpha) loaded injectable sustained release microspheres and to evaluate its release behavior, bioactivities in vitro as well as its pharmacodynamics in vivo, Talpha1 loaded microspheres was prepared with poly ( lactic-co-glycolic acid) (PLGA) as carrier material by double emulsion (W/O/W) method. Physical and chemical properties of microspheres, such as mean diameter, The release behavior and its influencing factors were morphology and drug loading were evaluated. evaluated by HPLC determination. The bioactivity of Talpha1 in the course of encapsulation process and in vitro release ware evaluated by CCK-8 method. The ratio of CD4+/CD8+ in blood was determined with flow cytometry and the pharmacodynamics of Ta, loaded microspheres was evaluated by the change of CD4+/ CD8+. Microspheres with good shape and dispersive quality were prepared. The drug entrapment efficiency of two optimizing prescriptions containing 5% NaCl and 10% glucose as outer water phase were 87. 8% and 90. 2% , respectively. The cumulated release in one month is up to 90%. The bioactivity of Talpha was conserved with glucose as outer water phase, but in the course of in vitro release, the specific activity of Talpha in the microspheres decreased a little. Talpha microspheres can increase significantly the immunity of immuno-suppressed rats. Talpha can be encapsulated in injectable microspheres to yield one-month continuous release when using biodegradable polymers PLGA as carrier material, and this technique will have a favorable perspective in the near future.
Zhu
Yan
Y
School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
Lu
Ying
Y
Zhong
Yan-qiang
YQ
D000818:Animals; D001682:Biological Availability; D016516:CD4-CD8 Ratio; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding / Q000379:methods*; D007267:Injections; D019344:Lactic Acid / Q000737:chemistry; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D000077596:Thymalfasin; D013947:Thymosin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D013947:Thymosin; D000077596:Thymalfasin