Lipid-core nanocapsules are an alternative to the pulmonary delivery and to increase the stability of statins

被引：11

作者：

Lorenzoni, Ricardo ^{[1
,5
]}

Cordenonsi, Leticia Malgarim ^{[1
,2
]}

Davies, Samuel ^{[1
,2
]}

Antonow, Michelli Barcelos ^{[1
,3
]}

Medina Diedrich, Aline Scheinder ^{[1
]}

Santos, Cayane Genro ^{[1
]}

Vitalis, Graciela Schneider ^{[1
]}

Garrastazu, Gabriela ^{[4
]}

Buttini, Francesca ^{[4
]}

Sonvico, Fabio ^{[4
]}

Gomes, Patricia ^{[1
]}

Raffin, Renata Platcheck ^{[1
]}

机构：

[1] Franciscan Univ, Nanosci Postgrad Program, Rua Andradas 1614, BR-97010032 Santa Maria, RS, Brazil

[2] Fed Univ Rio Grande do Sul State, Pharmaceut Sci Postgrad Program, Porto Alegre, RS, Brazil

[3] Fed Univ Rio Grande do Sul State, Pharmaceut Nanotechnol Postgrad Program, Porto Alegre, RS, Brazil

[4] Univ Parma, Fac Pharm, Parma, Italy

[5] Univ Santiago de Compostela, Mol Med & Chron Dis Res Ctr, Santiago De Compostela, Spain

来源：

JOURNAL OF MICROENCAPSULATION | 2019年 / 36卷 / 04期

关键词：

Nanocapsules; pulmonary delivery; HPLC; simvastatin; lovastatin; DRUG-INTERACTIONS; HPLC METHOD; CYTOTOXICITY; KINETICS; FORMULATION; DOXORUBICIN; SYSTEM; RISK;

D O I：

10.1080/02652048.2019.1624849

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Aims: Lipid-core nanocapsules (LNCs) loaded with simvastatin (SV, SV-LNC) or lovastatin (LV, LV-LNC) were formulated for pulmonary administration. Methods: The LNC suspensions were characterized physicochemically, their stability was evaluated, and drug delivery by the pulmonary route was tested in vitro. Results: The loaded LNCs had a particle size close to 200 nm, a low polydispersity index, and a zeta potential around -20 mV. The encapsulation efficiency was high for SV (99.21 +/- 0.7%) but low for LV (20.34 +/- 1.2%). SV release from nanocapsules was slower than it was from SV in solution, with a monoexponential release profile, and the drug emitted and aerosol output rate was higher for SV-LNCs (1.58 mu g/s) than for SV in suspension (0.54 mu g/s). Conclusions: SV-LNCs had a median aerodynamic diameter of 3.51 mu m and a highly respirable fraction (61.9%), indicating that nanoparticles are a suitable system for efficient delivery of simvastatin to the lung.

引用

页码：317 / 326

页数：10

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