Comparative study of liposomes, transfersomes and ethosomes as carriers for improving topical delivery of celecoxib

被引:131
作者
Bragagni, Marco [1 ]
Mennini, Natascia [1 ]
Maestrelli, Francesca [1 ]
Cirri, Marzia [1 ]
Mura, Paola [1 ]
机构
[1] Univ Florence, Fac Pharm, Dept Pharmaceut Sci, Florence, Italy
关键词
Liposomes; transfersomes; ethosomes; skin delivery; skin penetration; celecoxib; NONMELANOMA SKIN-CANCER; TRANSDERMAL DELIVERY; DEFORMABLE LIPOSOMES; STRATUM-CORNEUM; PENETRATION; FORMULATION; PERMEATION; OPTIMIZATION; ENHANCEMENT; EFFICACY;
D O I
10.3109/10717544.2012.724472
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
Topical administration of celecoxib proved to be an effective mean of preventing skin cancer development and improving anticancer drugs effectiveness in skin tumors treatment. The aim of this study was the development of an effective topical formulation of celecoxib, able to promote drug skin delivery, providing its in depth penetration through the skin layers. Three kinds of vesicular formulations have been investigated as drug carriers: liposomes containing a surfactant, or transfersomes and ethosomes, containing suitable edge activators. Firstly, the effect of membrane composition variations on the system performance has been evaluated for each vesicle type. Selected formulations were characterized for particle size, polydispersity index and encapsulation efficiency. The best formulations were subjected to ex vivo permeation studies through excised human skin. All vesicular formulations markedly (p < 0.001) improved the drug amount penetrated into the skin with respect to an aqueous suspension, from 2.0 to 6.5, up to 9.0 folds for liposomes, transfersomes and ethosomes, respectively. In particular, ethosomes containing Tween 20 as edge activator not only showed the best vesicle dimensions and homogeneity, and the highest encapsulation efficacy (54.4%), but also enabled the highest increase in drug penetration through the skin, probably due to the simultaneous presence in their composition of ethanol and Tween 20, both acting as permeation enhancers. Therefore, among the various vesicular formulations examined in the study, Tween 20-ethosomes can be considered the most promising one as carrier for topical celecoxib applications aimed to prevent skin cancer development and increase the anticancer drugs effectiveness against skin tumors.
引用
收藏
页码:354 / 361
页数:8
相关论文
共 40 条
[1]
[Anonymous], 2011, GLOB CANC FACTS FIG, V2nd
[2]
Liposomal formulations of prilocaine: effect of complexation with hydroxypropyl-β-cyclodextrin on drug anesthetic efficacy [J].
Bragagni, Marco ;
Maestrelli, Francesca ;
Mennini, Natascia ;
Ghelardini, Carla ;
Mura, Paola .
JOURNAL OF LIPOSOME RESEARCH, 2010, 20 (04) :315-322
[3]
Transfersomes, liposomes and other lipid suspensions on the skin: Permeation enhancement, vesicle penetration, and transdermal drug delivery [J].
Cevc, G .
CRITICAL REVIEWS IN THERAPEUTIC DRUG CARRIER SYSTEMS, 1996, 13 (3-4) :257-388
[4]
New, highly efficient formulation of diclofenac for the topical, transdermal administration in ultradeformable drug carriers, Transfersomes [J].
Cevc, G ;
Blume, G .
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, 2001, 1514 (02) :191-205
[5]
Characterization of solid-state forms of celecoxib [J].
Chawla, G ;
Gupta, P ;
Thilagavathi, R ;
Chakraborti, AK ;
Bansal, AK .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2003, 20 (03) :305-317
[6]
Carriers for skin delivery of trihexyphenidyl HCl: ethosomes vs. liposomes [J].
Dayan, N ;
Touitou, E .
BIOMATERIALS, 2000, 21 (18) :1879-1885
[7]
Melatonin loaded ethanolic liposomes: Physicochemical characterization and enhanced transdermal delivery [J].
Dubey, VaIbhav ;
Mishra, Dinesh ;
Jain, N. K. .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2007, 67 (02) :398-405
[8]
Liposomes and skin: From drug delivery to model membranes [J].
El Maghraby, G. M. ;
Barry, B. W. ;
Williams, A. C. .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2008, 34 (4-5) :203-222
[9]
Deformable liposomes and ethosomes as carriers for skin delivery of ketotifen [J].
Elsayed, M. M. A. ;
Abdallah, O. Y. ;
Naggar, V. F. ;
Khalafallah, N. M. .
PHARMAZIE, 2007, 62 (02) :133-137
[10]
Deformable liposomes and ethosomes: Mechanism of enhanced skin delivery [J].
Elsayed, Mustafa M. A. ;
Abdallah, Ossama Y. ;
Naggar, Viviane F. ;
Khalafallah, Nawal M. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2006, 322 (1-2) :60-66