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https://www.riss.kr/link?id=A19744207
2002
-
500
SCIE,SCOPUS,KCI등재
학술저널
104-113(10쪽)
0
상세조회0
다운로드다국어 초록 (Multilingual Abstract)
The effects of enzyme inhibitors and penetration enhancers on the permeation of leucine enkephalin (Leu-Enk) and its synthetic analog, [D-ala^2]-leucine enkephalinamide (YAGFL) across the nasal, rectal and vaginal mucosae were evaluated. Enzyme inhibi...
The effects of enzyme inhibitors and penetration enhancers on the permeation of leucine enkephalin (Leu-Enk) and its synthetic analog, [D-ala^2]-leucine enkephalinamide (YAGFL) across the nasal, rectal and vaginal mucosae were evaluated. Enzyme inhibitors and penetration enhancers employed for Leu-Enk permeation study were amastatin (AM), thimerosal (TM) and ethylenediaminetetraacetic acid disodium salt (EDTA), and sodium taurodihydrofusidate (STDHF). Those for YAGFL permeation study were TM, benzalkonium chloride (BC) and EDTA, and STDHF, sodium deoxycholate (SDC), sodium glycholate (SGC), glycyrrhizic acid ammonium salt (GAA), L-α-lysophosphatidylcholine (LPC) and mixed micelle (MM, STDHF : linoleic acid = 15 mM : 5 mM), The addition of TM alone on the donor and receptor solutions for Leu-Enk permeation study across all the three kinds of mucosae failed to inhibit the degradation; it completely degraded in 6 hrs, and no permeation occurred. However, with addition of three kinds of inhibitors together, the fluxes across nasal, rectal and vaginal mucosae were 20.7±2.5, 0.3±0.05 and 1.4±0.5 ㎍/㎠/hr, respectively. Moreover, the addition of STDHF in the presence of the above three inhibitors enhanced permeation across nasal, rectal and vaginal mucosae 1.3, 15 and 1.3 times, respectively. YAGFL also degraded in the donor and receptor solutions rapidly as time went. With mixed inhibitors of TM and EDTA, the percents of YAGFL remaining in the donor solutions facing nasal, rectal and vaginal mucosae were 69.7, 69.8 and 79.8%, respectively; the percent permeated increased to 10, 2.1 and 5.7%, respectively. The addition of STDHF in the presence of either BC/EDTA or TM/EDTA increased the permeation 2.2, 11.0 and 2.9 times, and 2.21, 14.0 and 2.7 times for nasal, rectal and vaginal mucosae, respectively. With SDC, SGC, GAA, LPC and MM in the presence of TM/EDTA increased permeation; especially, they increased permeation across vaginal mucosae effectively, and the enhancement factors were 12.5, 7.6, 8.7, 5.7 and 5.5, respectively. The degradation extent of YAGFL was correlated with protein concentrations in the epidermal and serosal extracts. The flux of YAGFL across nasal mucosa increased dose-dependently.
Up - regulation of Heme Oxygenase - 1 Expression by cAMP - elevating Agents in RAW 264.7 cells
조건적 불사화 흰쥐 뇌 모세혈관 내피세포주에서 Taurine 수송 특성