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Caproyl-Modified G2 PAMAM Dendrimer (G2-AC) Nanocomplexes Increases the Pulmonary Absorption of Insulin.
AAPS PharmSciTech. 2019 Aug 27; 20(7):298.AP

Abstract

We aimed to investigate the absorption-enhancing effect (AEE) of caproyl-modified G2 PAMAM dendrimer (G2-AC) on peptide and protein drugs via the pulmonary route. In this study, G2 PAMAM dendrimer conjugates modified with caproic acid was synthesized, the pulmonary absorption of insulin as models with or without G2-AC were evaluated. The results indicated that G2-AC6 exhibited a greatest AEE for insulin in various caproylation levels of G2-AC. G2-AC6 could significantly enhance the absorption of insulin, and the AEE of G2-AC6 was concentration-dependent. In toxicity tests, G2-AC6 displayed no measurable cytotoxicity to the pulmonary membranes over a concentration range from 0.1% (w/v) to 1.0% (w/v). Measurements of the TEER and permeability showed that G2-AC6 significantly reduced the TEER value of CF and increased its Papp value. The results suggested that G2-AC6 could cross epithelial cells by means of a combination of paracellular and transcellular pathways. These findings suggested G2-AC6 at lower concentrations (below 1.0%, w/v) might be promising absorption enhancers for increasing the pulmonary absorption of peptide and protein drugs.

Authors+Show Affiliations

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

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31456109

Citation

Yan, Chengyun, et al. "Caproyl-Modified G2 PAMAM Dendrimer (G2-AC) Nanocomplexes Increases the Pulmonary Absorption of Insulin." AAPS PharmSciTech, vol. 20, no. 7, 2019, p. 298.
Yan C, Gu J, Lv Y, et al. Caproyl-Modified G2 PAMAM Dendrimer (G2-AC) Nanocomplexes Increases the Pulmonary Absorption of Insulin. AAPS PharmSciTech. 2019;20(7):298.
Yan, C., Gu, J., Lv, Y., Shi, W., Wang, Y., Liao, Y., & Deng, Y. (2019). Caproyl-Modified G2 PAMAM Dendrimer (G2-AC) Nanocomplexes Increases the Pulmonary Absorption of Insulin. AAPS PharmSciTech, 20(7), 298. https://doi.org/10.1208/s12249-019-1505-x
Yan C, et al. Caproyl-Modified G2 PAMAM Dendrimer (G2-AC) Nanocomplexes Increases the Pulmonary Absorption of Insulin. AAPS PharmSciTech. 2019 Aug 27;20(7):298. PubMed PMID: 31456109.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Caproyl-Modified G2 PAMAM Dendrimer (G2-AC) Nanocomplexes Increases the Pulmonary Absorption of Insulin. AU - Yan,Chengyun, AU - Gu,Jiwei, AU - Lv,Yuguang, AU - Shi,Weiguo, AU - Wang,Yuefeng, AU - Liao,Ying, AU - Deng,Yueyi, Y1 - 2019/08/27/ PY - 2019/06/16/received PY - 2019/08/05/accepted PY - 2019/8/29/entrez PY - 2019/8/29/pubmed PY - 2019/12/4/medline KW - Caproyl-modified G2 PAMAM dendrimer KW - absorption enhancer KW - insulin KW - membrane toxicity KW - pulmonary absorption SP - 298 EP - 298 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 20 IS - 7 N2 - We aimed to investigate the absorption-enhancing effect (AEE) of caproyl-modified G2 PAMAM dendrimer (G2-AC) on peptide and protein drugs via the pulmonary route. In this study, G2 PAMAM dendrimer conjugates modified with caproic acid was synthesized, the pulmonary absorption of insulin as models with or without G2-AC were evaluated. The results indicated that G2-AC6 exhibited a greatest AEE for insulin in various caproylation levels of G2-AC. G2-AC6 could significantly enhance the absorption of insulin, and the AEE of G2-AC6 was concentration-dependent. In toxicity tests, G2-AC6 displayed no measurable cytotoxicity to the pulmonary membranes over a concentration range from 0.1% (w/v) to 1.0% (w/v). Measurements of the TEER and permeability showed that G2-AC6 significantly reduced the TEER value of CF and increased its Papp value. The results suggested that G2-AC6 could cross epithelial cells by means of a combination of paracellular and transcellular pathways. These findings suggested G2-AC6 at lower concentrations (below 1.0%, w/v) might be promising absorption enhancers for increasing the pulmonary absorption of peptide and protein drugs. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/31456109/Caproyl_Modified_G2_PAMAM_Dendrimer__G2_AC__Nanocomplexes_Increases_the_Pulmonary_Absorption_of_Insulin_ L2 - https://dx.doi.org/10.1208/s12249-019-1505-x DB - PRIME DP - Unbound Medicine ER -