Solubility and transdermal permeation properties of a dehydroepiandrosterone cyclodextrin complex from hydrophilic and lipophilic vehicles

被引:29
作者
Ceschel, G
Bergamante, V
Maffei, P
Borgia, SL
Calabrese, V
Biserni, S
Ronchi, C
机构
[1] Univ Bologna, Dept Pharmaceut Sci, I-40127 Bologna, Italy
[2] MonteRes SRL, Milan, Italy
关键词
alpha-cyclodextrin; dehydroepiandrosterone; enhancer effect; microemulsion; solubility; transdermal permeation;
D O I
10.1080/10717540500176563
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
The permeation ability of a compound is due principally to its concentration in the vehicle and to its aptitude to cross the stratum corneum of the skin. In this work ex-vivo permeation studies on newly developed formulations containing dehydroepiandrosterone (DHEA) were carried out to investigate vehicles that increase drug permeation through the skin. To enhance the solubility of DHEA, its complex form with a-cyclodextrin was used. In addition, the two forms (pure drug and complex form) were introduced in hydrophilic (water), lipophilic (paraffin oil), and microemulsion vehicles to evaluate the synergic effect of cyclodextrins and microemulsion vehicles on solubility and permeation. From the results, DHEA solubility is notably conditioned by the type of the vehicle used: the highest solubilities (both for pure and complex drug forms) were obtained with microemulsion, followed by paraffin oil and water. Moreover, in all the studied vehicles, the c-DHEA was more soluble than DHEA. Permeation profile fluxes showed very interesting differences. That reflect the varying drug forms (pure drug and complex form), vehicles used, and drug concentrations in the vehicles. The major flux was obtained in complex of DHEA with alpha-cyclodextrins in the microemulsion vehicle. Therefore, this type of vehicle and drug form would be very useful in the development of a topical formulation containing DHEA.
引用
收藏
页码:275 / 280
页数:6
相关论文
共 25 条
[1]
Physicochemical investigations on microemulsification of eucalyptol and water in presence of polyoxyethylene (4) lauryl ether (Brij-30) and ethanol [J].
Acharya, A ;
Sanyal, SK ;
Moulik, SP .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 229 (1-2) :213-226
[2]
Skin permeation study of dehydroepiandrosterone (DHEA) compared with its α-cyclodextrin complex form [J].
Ceschel, GC ;
Mora, PC ;
Borgia, SL ;
Maffei, P ;
Ronchi, C .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2002, 91 (11) :2399-2407
[3]
In vitro permeation through porcine buccal mucosa of Salvia desoleana Atzei & Picci essential oil from topical formulations [J].
Ceschel, GC ;
Maffei, P ;
Moretti, MDL ;
Demontis, S ;
Peana, AT .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 195 (1-2) :171-177
[4]
CESCHEL GC, 1999, FARM VESTN, V50, P297
[5]
Water-in-oil microemulsions containing medium-chain fatty acids salts: Formulation and intestinal absorption enhancement evaluation [J].
Constantinides, PP ;
Welzel, G ;
Ellens, H ;
Smith, PL ;
Sturgis, S ;
Yiv, SH ;
Owen, AB .
PHARMACEUTICAL RESEARCH, 1996, 13 (02) :210-215
[6]
Formulation study for the antitumor drug camptothecin: liposomes, micellar solutions and a microemulsion [J].
Cortesi, R ;
Esposito, E ;
Maietti, A ;
Menegatti, E ;
Nastruzzi, C .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 159 (01) :95-103
[7]
Inclusion complex of piroxicam with β-cyclodextrin and incorporation in hexadecyltrimethylammonium bromide based microemulsion [J].
Dalmora, MEA ;
Oliveira, AG .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1999, 184 (02) :157-164
[8]
PERCUTANEOUS ABSORPTION - RELEVANCE OF INVITRO DATA [J].
FRANZ, TJ .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1975, 64 (03) :190-195
[9]
INVITRO SKIN PERMEATION TECHNIQUES [J].
FRIEND, DR .
JOURNAL OF CONTROLLED RELEASE, 1992, 18 (03) :235-248
[10]
THE EFFECTS OF CYCLODEXTRINS ON DRUG ABSORPTION .1. INVITRO OBSERVATIONS [J].
FRIJLINK, HW ;
SCHOONEN, AJM ;
LERK, CF .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 49 (02) :91-102