Monoolein-based cubic liquid crystalline systems were formulated for the local delivery of oregonin and hirsutanonol for the treatment of atopic dermatitis. The liquid crystalline phase and its nanodispersion containing drugs were prepared. The skin permeation and deposition properties of the drugs ...
Monoolein-based cubic liquid crystalline systems were formulated for the local delivery of oregonin and hirsutanonol for the treatment of atopic dermatitis. The liquid crystalline phase and its nanodispersion containing drugs were prepared. The skin permeation and deposition properties of the drugs were examined in normal and delipidized rat skin. The proportion of oregonin (%) deposited in normal skin after topical administration of the drugs in the form of aqueous solution, cubic phase or cubic nanodispersions were $1.53\;{\pm}\;0.46$, $3.62\;{\pm}\;0.17$ and $5.13\;{\pm}\;0.73$, and those of hirsutanonol were $2.46\;{\pm}\;0.02$, $5.44\;{\pm}\;0.27$ and $17.28\;{\pm}\;2.19$, respectively. The greater lipophilicity and thus greater skin affinity of hirsutanonol than oregonin contributed the greater amount of skin deposition. The monoolein-based liquid crystalline phases significantly increased the amount of both drugs permeated and deposited. Approximately 3.2, 2.1 and 3.0 times greater amount of oregonin, and 3.4, 2.1 and 2.2 times greater amount of hirsutanonol were deposited in delipidized skin after administration of each drug in the form of aqueous solution, cubic phase and cubic nanodispersions system, respectively, because of lowered barrier function of the delipidized skin. In this study, the effects of drug property, vehicles type and skin condition on skin deposition and permeation properties of drug were examined and concluded that monoolein-based liquid crystalline systems would be a promising formulation for the local delivery of drugs.
Monoolein-based cubic liquid crystalline systems were formulated for the local delivery of oregonin and hirsutanonol for the treatment of atopic dermatitis. The liquid crystalline phase and its nanodispersion containing drugs were prepared. The skin permeation and deposition properties of the drugs were examined in normal and delipidized rat skin. The proportion of oregonin (%) deposited in normal skin after topical administration of the drugs in the form of aqueous solution, cubic phase or cubic nanodispersions were $1.53\;{\pm}\;0.46$, $3.62\;{\pm}\;0.17$ and $5.13\;{\pm}\;0.73$, and those of hirsutanonol were $2.46\;{\pm}\;0.02$, $5.44\;{\pm}\;0.27$ and $17.28\;{\pm}\;2.19$, respectively. The greater lipophilicity and thus greater skin affinity of hirsutanonol than oregonin contributed the greater amount of skin deposition. The monoolein-based liquid crystalline phases significantly increased the amount of both drugs permeated and deposited. Approximately 3.2, 2.1 and 3.0 times greater amount of oregonin, and 3.4, 2.1 and 2.2 times greater amount of hirsutanonol were deposited in delipidized skin after administration of each drug in the form of aqueous solution, cubic phase and cubic nanodispersions system, respectively, because of lowered barrier function of the delipidized skin. In this study, the effects of drug property, vehicles type and skin condition on skin deposition and permeation properties of drug were examined and concluded that monoolein-based liquid crystalline systems would be a promising formulation for the local delivery of drugs.
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문제 정의
And monoolein systems, particularly nanodispersion system considerably increased the skin deposition and permeation of both oregonin and hirsutanonol in normal and delipidized skin. This study shows that topical delivery of oregonin and hirsutanonol could be significantly enhanced via monoolein-based systems.
제안 방법
The aims of the present study were to formulate cubic crystalline phase or its nanoparticle system of oregonin and hirsutanonol and to investigate the localization factors for local skin delivery of oregonin and hirsutanonol. The effects of lipophilicity of drug, vehicle type and skin condition on skin permeation and deposition of the drugs were evaluated using the rat skin mounted in a Franz diffusion cells.
대상 데이터
Sprague-Dawley male rats (6 to 8 weeks old) were obtained from Hanlim Experimental Animal Center (Hwasung, Korea). The animals were sacrificed by overdose inhalation of chloroform.
The cumulative amount of drug permeated from excised rat skin into the receptor medium and deposited in excised rat skin was determined by HPLC. The HPLC system consisted of a quaternary pump (Hitachi, L-2130), an autosampler (Hitachi, L-2200), a column oven (Hitachi, L-2300), and a UV/VIS detector (Hitachi, L-2400, Japan) set to 280nm. The C18 column (150 mm 4.
이론/모형
Monoolein-based liquid crystalline systems were formulated for the effective skin delivery of oregonin and hirsutanonol. And the effects of lipophilicity of drugs, vehicles type and skin conditions on the localization of drug were evaluated in normal and delipidized rat skin using Franz diffusion model. The greater lipophilicity and thus higher skin affinity of hirsutanonol than oregonin attributed the greater amount of skin.
Physical characteristics of the cubic nanodispersions (size and size distribution, polydispersity index, and zeta potential) were determined by dynamic light scattering (DLS) method with Zetasizer Nano-ZS (Mal.,ern instrument, Worcestershire, UK). The measurements were repeated three times for each sample.
성능/효과
And the proportions (%) of oregonin deposited in delipidized skin from the aqueous solution, cubic phase or cubic nanodispersions were 4.88 ± 1.01, 7.51 ± 2.05 and 15.37 ± 0.39, respectively and those of hirsutanonol from aqueous solution, cubic phase or cubic nanodispersions were 8.42 ± 0.39, 11.56 ± 0.76 and 38.62 ± 0.88, respectively. Approximately 3.
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