Effect of cyclodextrins on the complexation and nasal permeation of melatonin.
Effect of cyclodextrins on the complexation and nasal permeation of melatonin.
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DOI：
10.1080/10717540802006922
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发表时间：
2008-08
期刊：
影响因子：
6
通讯作者：
Singh M
中科院分区：
文献类型：
--
作者：
Babu RJ;Dayal P;Singh M
研究了褪黑素（MT）与改性环糊精（CD）的包合作用，以提高MT的溶解度和鼻粘膜吸收。采用相溶解度和差示扫描量热法研究了MT与羟丙基βCD（HPβCD）和无规甲基化βCD（RMβCD）包合物的形成过程。相溶解度数据表明MT与CD的溶解度线性增加，证明了Higuchi的AL型相溶解度曲线。使用改进的非静态扩散装置研究CD对MT穿过EpiAirway™-100培养物的渗透的影响。CD以不同浓度与1%w/v微粉化MT悬浮液在羟丙基甲基纤维素（HPMC）载体中一起使用。在低CD浓度（1%w/v）下，MT从HPMC制剂的渗透显著增加（125%，p < .001）。然而，当CD以相对高的浓度使用时，渗透显著降低（HPβCD为5 - 10%w/v浓度，RMβCD为10%w/v浓度，p <0.001）。所有的组织都是活的，在渗透实验结束时具有良好的组织完整性，如通过甲基噻唑四唑测定和跨上皮电阻测量所测量的。结果表明，MT与HPβCD和RMβCD在溶液和固体状态下均形成包合物。发现1%w/v浓度的HPβCD和RMβCD均能改善来自HPMC凝胶制剂的MT的鼻渗透性。
The inclusion complexation of melatonin (MT) with modified cyclodextrins (CDs) was studied with an objective of improving the solubility and nasal absorption of MT. The formation of inclusion complex of MT with Hydroxypropyl βCD (HPβCD) and randomly methylated βCD (RMβCD) was characterized in solution and solid states by phase solubility and differential scanning calorimetry analyses. The phase solubility data indicate a linear increase in the solubility of MT with CDs demonstrating Higuchi’s AL-type phase solubility profiles. The effect of CDs on the permeation of MT across EpiAirway™-100 cultures was studied using a modified nonstatic diffusion setup. CDs were employed at different concentrations with 1% w/v micronized MT suspension in hydroxypropyl methyl cellulose (HPMC) vehicle. At low CD concentrations (1% w/v), the permeation of MT from HPMC formulation was significantly increased (125%, p < .001). However, the permeation was significantly reduced when CDs were used at relatively high concentrations (5 to 10% w/v concentration for HPβCD and 10% w/v concentration for RMβCD, p < .001). All the tissues were viable with good tissue integrity at the end of permeation experiments, as measured by methylthiazoletetrazolium assay and transepithelial electrical resistance measurements. In conclusion, formation of inclusion complex of MT with HPβCD and RMβCD was demonstrated in solution and solid state. Both HPβCD and RMβCD at 1% w/v concentration were found to improve the nasal permeability of MT from HPMC gel formulations.
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影响因子：
7.4
作者：
Feng, Z;Zhang, JT
通讯作者：
Zhang, JT
影响因子：
5.8
作者：
Sinswat, P;Tengamnuay, P
通讯作者：
Tengamnuay, P
DOI：
10.1111/j.1749-6632.1985.tb11811.x
发表时间：
1985-09-20
影响因子：
5.2
作者：
WALDHAUSER, F;DIETZEL, M
通讯作者：
DIETZEL, M
影响因子：
3.8
作者：
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通讯作者：
Costantino, HR
影响因子：
5.8
作者：
Babu, RJ;Pandit, JK
通讯作者：
Pandit, JK