Tags

Type your tag names separated by a space and hit enter

Improved intestinal absorption of water-soluble drugs by acetylation of G2 PAMAM dendrimer nanocomplexes in rat.
Drug Deliv Transl Res. 2017 06; 7(3):408-415.DD

Abstract

In search of an effective and less toxic absorption enhancer, we synthesized primary amine acetylation of generation 2 polyamidoamine (G2 PAMAM) dendrimer (Ac-G2) by the reaction of G2 PAMAM dendrimer with acetic anhydride, and evaluated the effects of Ac-G2 on the intestinal absorption of poorly absorbable water-soluble drugs using an in situ closed-loop method in rats. The results indicated that Ac50-G2 had a greatest absorption enhancing effect for 5(6)-carboxyfluorescein (CF) in various acetylation levels of G2 PAMAM dendrimers. Ac50-G2 with various concentrations (0.1-1.0%, w/v) could significantly improve the intestinal absorption of alendronate, CF, and fluorescein isothiocyanate-labeled dextrans (FD4), although they did not enhance the absorption of macromolecular drug of FD10, and the absorption enhancement effect of Ac50-G2 was concentration-dependent. Furthermore, we examined the intestinal membrane damage with or without Ac50-G2. The results displayed Ac50-G2 at lower concentrations (0.1-0.5%, w/v) did not cause any observed toxic effect to the intestinal membranes. These findings suggested Ac50-G2 at lower concentrations (below 0.5%, w/v) might be promising as an effective and safe absorption enhancers to promote the intestinal absorption of poorly absorbable drugs.

Authors+Show Affiliations

College of Pharmacy|, Guilin Medical University, Guilin,, 541004, China. hademan@126.com. First Affiliated Hospital of Jiamusi University, Jiamusi University, Jiamusi, 154000, China. hademan@126.com.First Affiliated Hospital of Jiamusi University, Jiamusi University, Jiamusi, 154000, China.College of Pharmacy, Jiamusi University, Jiamusi, 154000, China.College of Pharmacy, Jiamusi University, Jiamusi, 154000, China.First Affiliated Hospital of Jiamusi University, Jiamusi University, Jiamusi, 154000, China.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

28303451

Citation

Yan, Chengyun, et al. "Improved Intestinal Absorption of Water-soluble Drugs By Acetylation of G2 PAMAM Dendrimer Nanocomplexes in Rat." Drug Delivery and Translational Research, vol. 7, no. 3, 2017, pp. 408-415.
Yan C, Gu J, Lv Y, et al. Improved intestinal absorption of water-soluble drugs by acetylation of G2 PAMAM dendrimer nanocomplexes in rat. Drug Deliv Transl Res. 2017;7(3):408-415.
Yan, C., Gu, J., Lv, Y., Shi, W., & Jing, H. (2017). Improved intestinal absorption of water-soluble drugs by acetylation of G2 PAMAM dendrimer nanocomplexes in rat. Drug Delivery and Translational Research, 7(3), 408-415. https://doi.org/10.1007/s13346-017-0373-8
Yan C, et al. Improved Intestinal Absorption of Water-soluble Drugs By Acetylation of G2 PAMAM Dendrimer Nanocomplexes in Rat. Drug Deliv Transl Res. 2017;7(3):408-415. PubMed PMID: 28303451.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improved intestinal absorption of water-soluble drugs by acetylation of G2 PAMAM dendrimer nanocomplexes in rat. AU - Yan,Chengyun, AU - Gu,Jiwei, AU - Lv,Yuguang, AU - Shi,Weiguo, AU - Jing,Hongying, PY - 2017/3/18/pubmed PY - 2018/2/16/medline PY - 2017/3/18/entrez KW - Absorption enhancer KW - Acetylation modification KW - G2 PAMAM dendrimer KW - Intestinal absorption KW - Poorly absorbable drugs SP - 408 EP - 415 JF - Drug delivery and translational research JO - Drug Deliv Transl Res VL - 7 IS - 3 N2 - In search of an effective and less toxic absorption enhancer, we synthesized primary amine acetylation of generation 2 polyamidoamine (G2 PAMAM) dendrimer (Ac-G2) by the reaction of G2 PAMAM dendrimer with acetic anhydride, and evaluated the effects of Ac-G2 on the intestinal absorption of poorly absorbable water-soluble drugs using an in situ closed-loop method in rats. The results indicated that Ac50-G2 had a greatest absorption enhancing effect for 5(6)-carboxyfluorescein (CF) in various acetylation levels of G2 PAMAM dendrimers. Ac50-G2 with various concentrations (0.1-1.0%, w/v) could significantly improve the intestinal absorption of alendronate, CF, and fluorescein isothiocyanate-labeled dextrans (FD4), although they did not enhance the absorption of macromolecular drug of FD10, and the absorption enhancement effect of Ac50-G2 was concentration-dependent. Furthermore, we examined the intestinal membrane damage with or without Ac50-G2. The results displayed Ac50-G2 at lower concentrations (0.1-0.5%, w/v) did not cause any observed toxic effect to the intestinal membranes. These findings suggested Ac50-G2 at lower concentrations (below 0.5%, w/v) might be promising as an effective and safe absorption enhancers to promote the intestinal absorption of poorly absorbable drugs. SN - 2190-3948 UR - https://www.unboundmedicine.com/medline/citation/28303451/Improved_intestinal_absorption_of_water_soluble_drugs_by_acetylation_of_G2_PAMAM_dendrimer_nanocomplexes_in_rat_ L2 - https://dx.doi.org/10.1007/s13346-017-0373-8 DB - PRIME DP - Unbound Medicine ER -