Thermal behavior and stability of biodegradable spray-dried microparticles containing triamcinolone


Autoria(s): SILVA-JUNIOR, Arnobio Antonio da; MATOS, Jivaldo Rosario de; FORMARIZ, Thalita Pedroni; ROSSANEZI, Gustavo; SCARPA, Maria Virginia; EGITO, Eryvaldo Socrates Tabosa do; OLIVEIRA, Anselmo Gomes de
Contribuinte(s)

UNIVERSIDADE DE SÃO PAULO

Data(s)

20/10/2012

20/10/2012

2009

Resumo

Thermal analysis has been widely used for obtaining information about drug-polymer interactions and for pre-formulation studies of pharmaceutical dosage forms. In this work, biodegradable microparticles Of Poly (D,L-lactide-co-glycolide) (PLGA) containing triamcinolone (TR) in various drug:polymer ratios were produced by spray drying. The main purpose of this study was to study the effect of the spray-drying process not only on the drug-polymer interactions but also on the stability of microparticles using differential scanning calorimetry (DSC), thermogravimetry (TG) and derivative thermogravimetry (DTG), X-ray analysis (XRD), and infrared spectroscopy (IR). The evaluation of drug-polymer interactions and the pre-formulation studies were assessed using the DSC, TG and DTG, and IR. The quantitative analysis of drugs entrapped in PLGA microparticles was performed by the HPLC method. The results showed high levels of drug-loading efficiency for all used drug: polymer ratio, and the polymorph used for preparing the microparticles was the form B. The DSC and TG/DTG profiles for drug-loaded microparticles were very similar to those for the physical mixtures of the components. Therefore, a correlation between drug content and the structural and thermal properties of drug-loaded PLGA microparticles was established. These data indicate that the spray-drying technique does not affect the physico-chemical stability of the microparticle components. These results are in agreement with the IR analysis demonstrating that no significant chemical interaction occurs between TR and PLGA in both physical mixtures and microparticles. The results of the X-ray analysis are in agreement with the thermal analysis data showing that the amorphous form of TR prevails over a small fraction of crystalline phase of the drug also present in the TR-loaded microparticles. From the pre-formulation studies, we have found that the spray-drying methodology is an efficient process for obtaining TR-loaded PLGA microparticles. (C) 2008 Elsevier B.V. All rights reserved.

FAPESP

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

CNPq

PADC-FCF

PADC-FCF

CAPES

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Identificador

INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.368, n.1/Fev, p.45-55, 2009

0378-5173

http://producao.usp.br/handle/BDPI/31225

10.1016/j.ijpharm.2008.09.054

http://dx.doi.org/10.1016/j.ijpharm.2008.09.054

Idioma(s)

eng

Publicador

ELSEVIER SCIENCE BV

Relação

International Journal of Pharmaceutics

Direitos

restrictedAccess

Copyright ELSEVIER SCIENCE BV

Palavras-Chave #Triamcinolone #PLGA microparticles #Spray drying #Thermal analysis #X-ray analysis #Thermal stability #DRUG-DELIVERY SYSTEMS #DICLOFENAC SODIUM #SOLID-STATE #PHYSICAL STABILITY #PLGA MICROSPHERES #DRYING TECHNIQUE #MACULAR EDEMA #PEG 6000 #INTRAVITREAL #RELEASE #Pharmacology & Pharmacy
Tipo

article

original article

publishedVersion