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Enhancement potential of sucrose laurate (L-1695) on intestinal absorption of water-soluble high molecular weight compounds.
Curr Drug Deliv. 2012 Sep; 9(5):487-94.CD

Abstract

PURPOSE

The potential of sucrose fatty acid esters (SEs) to enhance intestinal absorption was investigated in order to identify their utility for the intestinal absorption of water-soluble high molecular weight compounds.

METHODS

Fluorescein isothiocyanate-labeled dextran (FD) with a molecular weight (MW) of 4,000 (FD-4) was used as a model compound, and several SEs were tested as absorption enhancers. After FD-4 was administered intra-duodenally at 10 % (w/v) with the non-loop method in situ in rats in the absence or presence of SEs, the plasma concentration-time profiles of FD-4 were examined. As to sucrose laurate (L-1695), the relationship between concentration and enhancement effect was investigated. In addition, the enhancement effect after dosing into the different small intestinal regions, the effect on FDs with different MWs and the influence of N-acetyl-cysteine (NAC) co-existence were examined.

RESULTS

Low water-soluble SEs exhibited slight and/or slow absorption enhancement effects, while L-1695, being highly water-soluble, had good potential to enhance the absorption rate and extent. The enhancement effect became greater as the concentration of L1695 increased. L-1695 displayed high enhancement potential in wide intestinal areas. The enhancement effect of L-1695 (10 %, w/v) depended on MWs of FDs; the mean values of the area under the plasma concentration curve from 0-120 min (AUC0-120 mins) increased by 14 and 8 times for FD-4 and FD-10 (MW 10,000), while it was hardly changed as for FD-70 (MW 70,000). The enhancement effect of L-1695 (10 %, w/v) was similar to that of sodium caprate (10 %, w/v), and was influenced to some extent by the co-existence of NAC (5 %, w/v).

CONCLUSION

The absorption enhancement potential of SEs depended on their water-solubility. L-1695, being highly water-soluble, showed a good enhancement effect, and its absorption profiles were elucidated. This study proposes the possibility of SEs, in particular, L-1695, as intestinal absorption enhancers. As far as the present non-loop method is concerned, the intestinal damage was not observed macroscopically with the addition of L1695 at 2.5-20 % (w/v).

Authors+Show Affiliations

Department of Drug Delivery Research, Hoshi University, Ebara, Shinagawa-ku, Tokyo, Japan. onsihi@hoshi.ac.jpNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22520068

Citation

Onishi, Hiraku, et al. "Enhancement Potential of Sucrose Laurate (L-1695) On Intestinal Absorption of Water-soluble High Molecular Weight Compounds." Current Drug Delivery, vol. 9, no. 5, 2012, pp. 487-94.
Onishi H, Imura Y, Uchida M, et al. Enhancement potential of sucrose laurate (L-1695) on intestinal absorption of water-soluble high molecular weight compounds. Curr Drug Deliv. 2012;9(5):487-94.
Onishi, H., Imura, Y., Uchida, M., & Machida, Y. (2012). Enhancement potential of sucrose laurate (L-1695) on intestinal absorption of water-soluble high molecular weight compounds. Current Drug Delivery, 9(5), 487-94.
Onishi H, et al. Enhancement Potential of Sucrose Laurate (L-1695) On Intestinal Absorption of Water-soluble High Molecular Weight Compounds. Curr Drug Deliv. 2012;9(5):487-94. PubMed PMID: 22520068.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhancement potential of sucrose laurate (L-1695) on intestinal absorption of water-soluble high molecular weight compounds. AU - Onishi,Hiraku, AU - Imura,Yu, AU - Uchida,Minoru, AU - Machida,Yoshiharu, PY - 2011/11/25/received PY - 2012/01/23/revised PY - 2012/03/28/accepted PY - 2012/4/24/entrez PY - 2012/4/24/pubmed PY - 2013/2/6/medline SP - 487 EP - 94 JF - Current drug delivery JO - Curr Drug Deliv VL - 9 IS - 5 N2 - PURPOSE: The potential of sucrose fatty acid esters (SEs) to enhance intestinal absorption was investigated in order to identify their utility for the intestinal absorption of water-soluble high molecular weight compounds. METHODS: Fluorescein isothiocyanate-labeled dextran (FD) with a molecular weight (MW) of 4,000 (FD-4) was used as a model compound, and several SEs were tested as absorption enhancers. After FD-4 was administered intra-duodenally at 10 % (w/v) with the non-loop method in situ in rats in the absence or presence of SEs, the plasma concentration-time profiles of FD-4 were examined. As to sucrose laurate (L-1695), the relationship between concentration and enhancement effect was investigated. In addition, the enhancement effect after dosing into the different small intestinal regions, the effect on FDs with different MWs and the influence of N-acetyl-cysteine (NAC) co-existence were examined. RESULTS: Low water-soluble SEs exhibited slight and/or slow absorption enhancement effects, while L-1695, being highly water-soluble, had good potential to enhance the absorption rate and extent. The enhancement effect became greater as the concentration of L1695 increased. L-1695 displayed high enhancement potential in wide intestinal areas. The enhancement effect of L-1695 (10 %, w/v) depended on MWs of FDs; the mean values of the area under the plasma concentration curve from 0-120 min (AUC0-120 mins) increased by 14 and 8 times for FD-4 and FD-10 (MW 10,000), while it was hardly changed as for FD-70 (MW 70,000). The enhancement effect of L-1695 (10 %, w/v) was similar to that of sodium caprate (10 %, w/v), and was influenced to some extent by the co-existence of NAC (5 %, w/v). CONCLUSION: The absorption enhancement potential of SEs depended on their water-solubility. L-1695, being highly water-soluble, showed a good enhancement effect, and its absorption profiles were elucidated. This study proposes the possibility of SEs, in particular, L-1695, as intestinal absorption enhancers. As far as the present non-loop method is concerned, the intestinal damage was not observed macroscopically with the addition of L1695 at 2.5-20 % (w/v). SN - 1875-5704 UR - https://www.unboundmedicine.com/medline/citation/22520068/Enhancement_potential_of_sucrose_laurate__L_1695__on_intestinal_absorption_of_water_soluble_high_molecular_weight_compounds_ L2 - https://www.ingentaconnect.com/openurl?genre=article&issn=1567-2018&volume=9&issue=5&spage=487&aulast=Onishi DB - PRIME DP - Unbound Medicine ER -