Preparation and in vitro evaluation of liposomal/niosomal delivery systems for antipsoriatic drug dithranol

被引:221
作者
Agarwal, R
Katare, OP [1 ]
Vyas, SP
机构
[1] Punjab Univ, Univ Inst Pharmaceut Sci, Chandigarh 160014, India
[2] Sagar Univ, HS Gour Inst Pharmaceut Sci, Sagar, Madhya Pradesh, India
关键词
topical delivery; liposomes; niosomes; dithranol; entrapment efficiency; stability; skin-permeation;
D O I
10.1016/S0378-5173(01)00810-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Dithranol is one of the mainstays in the topical treatment of psoriasis. However. the use of dithranol in psoriatic condition is inconvenient and troublesome, as it has irritating, burning, staining and necrotizing effect on the normal as well as the diseased skin. The entrapment of drug in vesicles is viewed to help in the localized delivery of the drug and an improved availability of the drug at the site will reduce the dose and in turn, the dose-dependent side effects like irritation and staining. The investigations deal with critical parameters controlling the formulation and stabilization of dithranol loaded liposomes and niosomes. The entrapment efficiency of dithranol in liposomes was optimized by altering the proportion of phosphatidyl choline and cholesterol. and in case of niosomes it was between Span 60 and cholesterol. Hydration and permeation mediums were also established keeping in view the poor solubility and stability of dithranol. The mean liposome and niosomes sizes were 4 +/- 1.25 and 5 +/- 1.5 Am, respectively. The drug-leakage study carried out at different temperatures of 4-8. 25 +/- 2 and 37 degreesC for a period of two months affirms that the drug leakage increased at a higher temperature. The in vitro permeation study using mouse abdominal skin shows significantly enhanced permeation with vesicles as indicated by flux of dithranol from liposomes (23.13 mug/cm(2)/h) and niosomes (7.78 mug/cm(2)/h) as compared with the cream base (4.10 mug/cm(2)/h). (C) 2001 Elsevier Science BN. All rights reserved.
引用
收藏
页码:43 / 52
页数:10
相关论文
共 20 条
[11]   IRRITATION, STAINING AND ANTIPSORIATIC ACTIVITY OF 10-ACYL ANALOGS OF ANTHRALIN [J].
MUSTAKALLIO, KK .
BRITISH JOURNAL OF DERMATOLOGY, 1981, 105 :23-27
[12]  
NEW RRC, 1990, LIPOSOMES PRACTICAL, P256
[13]  
Patel VB, 1999, J MICROENCAPSUL, V16, P357
[14]  
REDZINIAK G, 1996, MICROENCAPSULATION M
[15]   ANTIRESPIRATORY AND ANTIPROLIFERATIVE ACTIVITY OF ANTHRALIN IN CULTURED HUMAN KERATINOCYTES [J].
REICHERT, U ;
JACQUES, Y ;
GRANGERET, M ;
SCHMIDT, R .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1985, 84 (02) :130-134
[16]   Non-ionic surfactant based vesicles (niosomes) in drug delivery [J].
Uchegbu, IF ;
Vyas, SP .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1998, 172 (1-2) :33-70
[17]  
VLEUTEN CJM, 1996, ACTA DERM-VENER S, V76, P387
[18]   Influence of liposome bilayer fluidity on the transport of encapsulated substance into the skin as evaluated by EPR [J].
Vrhovnik, K ;
Kristl, J ;
Sentjurc, M ;
Smid-Korbar, J .
PHARMACEUTICAL RESEARCH, 1998, 15 (04) :525-530
[19]   THE RELEASE AND PERCUTANEOUS PERMEATION OF ANTHRALIN PRODUCTS, USING CLINICALLY INVOLVED AND UNINVOLVED PSORIATIC SKIN [J].
WANG, JCT ;
PATEL, BG ;
EHMANN, CW ;
LOWE, N .
JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, 1987, 16 (04) :812-821
[20]   PHARMACEUTICAL FORMULATIONS OF ANTHRALIN [J].
WHITEFIELD, M .
BRITISH JOURNAL OF DERMATOLOGY, 1981, 105 :28-32