Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules

Author(s)

Michalowski, Cecilia B. ^{[1, 2]} ; Arbo, Marcelo D. ^{[1, 3]} ; Altknecht, Louise ^[3] ; Anciuti, Andreia N. ^[4] ; Abreu, Angelica S. G. ^[5] ; Alencar, Luciana M. R. ^[5] ; Pohlmann, Adriana R. ^{[1, 6]} ; Garcia, Solange C. ^{[1, 3]} ; Guterres, Silvia S. ^{[1, 2]}

Affiliation

^[1] Univ Fed Rio Grande do Sul, Programa Posgrad Ciencias Farmaceut, Ave Ipiranga 2752, BR-90610000 Porto Alegre - Brazil

^[2] Univ Fed Rio Grande do Sul, Fac Farm, Dept Prod & Controle Medicamentos, Ave Ipiranga 2752, BR-90610000 Porto Alegre, RS - Brazil

^[3] Univ Fed Rio Grande do Sul, Lab Toxicol LATOX, Ave Ipiranga 2752, BR-90610000 Porto Alegre, RS - Brazil

^[4] Univ Fed Rio Grande do Sul, Inst Ciencias Basicas Saude, Dept Bioquim, Rua Ramiro Barcelos, 2600 Anexo, BR-90035003 Porto Alegre, RS - Brazil

^[5] Univ Fed Ceara, Dept Fis, Lab Microscopia Avancada, Campus Pici, BR-60455900 Fortaleza, Ceara - Brazil

^[6] Univ Fed Rio Grande do Sul, Inst Quim, Dept Quim Organ, PBox 15003, Ave Bento Goncalves 9500, BR-91501970 Porto Alegre, RS - Brazil

• Document type: Journal article
• Source: PHARMACEUTICS; v. 12, n. 1 JAN 2020.
• Web of Science Citations: 0

Abstract

Multi-wall lipid-core nanocapsule (MLNC) functionalized with captopril and nanoencapsulating furosemide within the core was developed as a liquid formulation for oral administration. The nanocapsules had mean particle size below 200 nm, showing unimodal and narrow size distributions with moderate dispersity (laser diffraction and dynamic light scattering). Zeta potential was inverted from -14.3 mV {[}LNC-Fur(0,5)] to +18.3 mV after chitosan coating. Transmission electron microscopy and atomic force microscopy showed spherical structures corroborating the nanometric diameter of the nanocapsules. Regarding the systolic pressure, on the first day, the formulations showed antihypertensive effect and a longer effect than the respective drug solutions. When both drugs were associated, the anti-hypertensive effect was prolonged. On the fifth day, a time effect reduction was observed for all treatments, except for the nanocapsule formulation containing both drugs {[}Capt(0.5)-Zn(25)-MLNC-Fur(0.45)]. For diastolic pressure, only Capt(0.5)-Zn(25)-MLNC-Fur(0.45) presented a significant difference (p < 0.05) on the first day. On the fifth day, both Capt(0.5)-MLNC-Fur(0.45) and Capt(0.5)-Zn(25)-MLNC-Fur(0.45) had an effect lasting up to 24 h. The analysis of early kidney damage marker showed a potential protection in renal function by Capt(0.5)-Zn(25)-MLNC-Fur(0.45). In conclusion, the formulation Capt(0.5)-Zn(25)-MLNC-Fur(0.45) proved to be suitable for hypertension treatment envisaging an important innovation. (AU)

• FAPESP's process: 14/50928-2 - INCT 2014: Pharmaceutical Nanotechnology: a transdisciplinary approach
• Grantee: Maria Vitória Lopes Badra Bentley
• Support Opportunities: Research Projects - Thematic Grants