Development and characterization of skin permeation retardants and enhancers: A comparative study of levothyroxine-loaded PNIPAM, PLA, PLGA and EC microparticles

被引:13
作者
Azarbayjani, Anahita Fathi [1 ,2 ]
Khu, Jia Vu [1 ]
Chan, Yew Weng [3 ]
Chan, Sui Yung [1 ]
机构
[1] Natl Univ Singapore, Dept Pharm, Singapore 117543, Singapore
[2] Urmia Univ Med Sci, Dept Med, Orumiyeh 5756115111, Iran
[3] Singapore Gen Hosp, Dept Anaesthesiol, Singapore 169608, Singapore
关键词
penetration enhancers; penetration retardants; ethyl cellulose; poly D; L lactide; poly (N-isopropylacrylamide); DRUG-DELIVERY SYSTEM; ETHYL CELLULOSE; STRATUM-CORNEUM; N-ISOPROPYLACRYLAMIDE; TABLETS; WATER; NANOPARTICLES; PLASTICIZERS; MICROSPHERES; COPOLYMERS;
D O I
10.1002/bdd.766
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Polymeric microparticles suitable for topical and transdermal delivery systems were studied using poly D,L lactide (PLA), poly D,L lactide co glycoside (PLGA), poly (N-isopropylacrylamide) (PNIPAM) and ethyl cellulose (EC). Drug encapsulation efficacy, microparticle stability and skin permeation studies of levothyroxine loaded microparticles were carried out using excised human skin, and the skin permeation pattern was observed using confocal laser scanning microscopy. It was found that ethyl cellulose microparticles had the highest drug encapsulation and minimal drug leakage during the 14week storage period. The PNIPAM microparticles had the lowest drug encapsulation efficiency and a fast degradation rate. The PLGA microparticles exhibited a temperature dependent drug leakage. Permeation studies using a flow-through diffusion cell indicated that the polymer transition temperature (T(g)) may influence the skin permeation rate of levothyroxine. Polyesters (PLA and PLGA) and PNIPAM acted as a skin penetration retardant and caused skin accumulation of the drug. These microparticles have potential use in skin formulations containing sunscreens and other active ingredients that are meant to be concentrated on the skin surface. However, skin permeation was observed from EC microparticles, therefore such polymers may be used as carriers in transdermal formulations to help achieve therapeutic concentrations of the drug in the plasma. Copyright (C) 2011 John Wiley & Sons, Ltd.
引用
收藏
页码:380 / 388
页数:9
相关论文
共 39 条
[1]   Skin permeation of propranolol from polymeric film containing terpene enhancers for transdermal use [J].
Amnuaikit, C ;
Ikeuchi, I ;
Ogawara, K ;
Higaki, K ;
Kimura, T .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2005, 289 (1-2) :167-178
[2]   KINETICS OF THYROXINE EPICUTANEOUS ABSORPTION [J].
ARDUINO, C ;
EANDI, M .
PHARMACOLOGICAL RESEARCH, 1989, 21 (01) :109-110
[3]  
Asbill Charles S., 2000, Pharmaceutical Science and Technology Today, V3, P36, DOI 10.1016/S1461-5347(99)00225-4
[4]   Preparation, characterization, cytotoxicity and transfection efficiency of poly(DL-lactide-co-glycolide) and poly(DL-lactic acid) cationic nanoparticles for controlled delivery of plasmid DNA [J].
Basarkar, Ashwin ;
Devineni, Dilip ;
Palaniappan, Ravi ;
Singh, Jagdish .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2007, 343 (1-2) :247-254
[5]   Physical characterization of the stratum corneum of an in vitro psoriatic skin model by ATR-FTIR and Raman spectroscopies [J].
Bernard, Genevieve ;
Auger, Michele ;
Soucy, Jacques ;
Pouliot, Roxane .
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS, 2007, 1770 (09) :1317-1323
[6]   Thermosensitive poly(N-isopropylacrylamide)-b-poly(ε-caprolactone) nanoparticles for efficient drug delivery system [J].
Choi, Changyong ;
Chae, Su Young ;
Nah, Jae-Won .
POLYMER, 2006, 47 (13) :4571-4580
[7]   PREPARATION OF POROUS AND NONPOROUS BIODEGRADABLE POLYMERIC HOLLOW MICROSPHERES [J].
CROTTS, G ;
PARK, TG .
JOURNAL OF CONTROLLED RELEASE, 1995, 35 (2-3) :91-105
[8]   Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion [J].
Crowley, MM ;
Schroeder, B ;
Fredersdorf, A ;
Obara, S ;
Talarico, M ;
Kucera, S ;
McGinity, JW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2004, 269 (02) :509-522
[9]   Topical application of acyclovir-loaded microparticles:: quantification of the drug in porcine skin layers [J].
de Jalón, EG ;
Blanco-Príeto, MJ ;
Ygartua, P ;
Santoyo, S .
JOURNAL OF CONTROLLED RELEASE, 2001, 75 (1-2) :191-197
[10]   Thermosensitive water-soluble copolymers with doubly responsive reversibly interacting entities [J].
Dimitrov, Ivaylo ;
Trzebicka, Barbara ;
Muller, Axel H. E. ;
Dworak, Andrzej ;
Tsvetanov, Christo B. .
PROGRESS IN POLYMER SCIENCE, 2007, 32 (11) :1275-1343