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Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats.
Nanomedicine. 2012 Jul; 8(5):740-7.N

Abstract

Candesartan cilexetil (CC) is widely used for the treatment of hypertension and heart failure, but it shows very poor aqueous solubility and very low oral absorption. In this work, CC-loaded solid lipid nanoparticles (CLNs) were successfully developed to improve the oral bioavailability. The physicochemical properties of CLNs were characterized, and the pharmacokinetic behavior of CLNs was evaluated in rats. CLNs exhibited nanometer-sized spherical particles with high entrapment efficiency (91.33%). The absorption of CLNs in the stomach was only 2.8% of that in intestine. Moreover, CLNs could be internalized into the enterocytes and then transported into the systemic circulation via the portal circulation and intestinal lymphatic pathway. The pharmacokinetic results indicated that the oral bioavailability of candesartan was obviously improved over 12-fold after incorporation into solid lipid nanoparticles. These results demonstrated that solid lipid nanoparticles have great potential for increasing oral bioavailability of lipophilic drugs such as CC.

FROM THE CLINICAL EDITOR

Candesartan cilexetil is a potent angiotensin receptor inhibitor with low bioavailability due to poor aqueous solubility. In this work, solid lipid nanoparticles were used to improve the oral bioavailability 12-fold compared to standard preparation in rats, suggesting that a similar approach might be effective in future human applications.

Authors+Show Affiliations

Center of Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

21930110

Citation

Zhang, Zhiwen, et al. "Solid Lipid Nanoparticles Loading Candesartan Cilexetil Enhance Oral Bioavailability: in Vitro Characteristics and Absorption Mechanism in Rats." Nanomedicine : Nanotechnology, Biology, and Medicine, vol. 8, no. 5, 2012, pp. 740-7.
Zhang Z, Gao F, Bu H, et al. Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats. Nanomedicine. 2012;8(5):740-7.
Zhang, Z., Gao, F., Bu, H., Xiao, J., & Li, Y. (2012). Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats. Nanomedicine : Nanotechnology, Biology, and Medicine, 8(5), 740-7. https://doi.org/10.1016/j.nano.2011.08.016
Zhang Z, et al. Solid Lipid Nanoparticles Loading Candesartan Cilexetil Enhance Oral Bioavailability: in Vitro Characteristics and Absorption Mechanism in Rats. Nanomedicine. 2012;8(5):740-7. PubMed PMID: 21930110.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats. AU - Zhang,Zhiwen, AU - Gao,Fang, AU - Bu,Huihui, AU - Xiao,Jisheng, AU - Li,Yaping, Y1 - 2011/09/17/ PY - 2010/11/28/received PY - 2011/06/27/revised PY - 2011/08/29/accepted PY - 2011/9/21/entrez PY - 2011/9/21/pubmed PY - 2013/1/1/medline SP - 740 EP - 7 JF - Nanomedicine : nanotechnology, biology, and medicine JO - Nanomedicine VL - 8 IS - 5 N2 - : Candesartan cilexetil (CC) is widely used for the treatment of hypertension and heart failure, but it shows very poor aqueous solubility and very low oral absorption. In this work, CC-loaded solid lipid nanoparticles (CLNs) were successfully developed to improve the oral bioavailability. The physicochemical properties of CLNs were characterized, and the pharmacokinetic behavior of CLNs was evaluated in rats. CLNs exhibited nanometer-sized spherical particles with high entrapment efficiency (91.33%). The absorption of CLNs in the stomach was only 2.8% of that in intestine. Moreover, CLNs could be internalized into the enterocytes and then transported into the systemic circulation via the portal circulation and intestinal lymphatic pathway. The pharmacokinetic results indicated that the oral bioavailability of candesartan was obviously improved over 12-fold after incorporation into solid lipid nanoparticles. These results demonstrated that solid lipid nanoparticles have great potential for increasing oral bioavailability of lipophilic drugs such as CC. FROM THE CLINICAL EDITOR: Candesartan cilexetil is a potent angiotensin receptor inhibitor with low bioavailability due to poor aqueous solubility. In this work, solid lipid nanoparticles were used to improve the oral bioavailability 12-fold compared to standard preparation in rats, suggesting that a similar approach might be effective in future human applications. SN - 1549-9642 UR - https://www.unboundmedicine.com/medline/citation/21930110/Solid_lipid_nanoparticles_loading_candesartan_cilexetil_enhance_oral_bioavailability:_in_vitro_characteristics_and_absorption_mechanism_in_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1549-9634(11)00353-4 DB - PRIME DP - Unbound Medicine ER -