Simvastatin-loaded solid lipid nanoparticles for enhanced anti-hyperlipidemic activity in hyperlipidemia animal model
- Authors
- Rizvi, Syed Zaki Husain; Shah, Fawad Ali; Khan, Namrah; Muhammad, Iftikhar; Ali, Khan Hashim; Ansari, Muhammad Mohsin; Din, Fakhar Ud; Qureshi, Omer Salman; Kim, Kyoung-Won; Choe, Yeong-Hwan; Kim, Jin-Ki; Zeb, Alam
- Issue Date
- Apr-2019
- Publisher
- ELSEVIER SCIENCE BV
- Keywords
- Simvastatin; HMG-CoA reductase; Solid lipid nanoparticles; Sustained release; Hyperlipidemia; Improved therapeutic efficiency
- Citation
- INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.560, pp.136 - 143
- Indexed
- SCIE
SCOPUS
- Journal Title
- INTERNATIONAL JOURNAL OF PHARMACEUTICS
- Volume
- 560
- Start Page
- 136
- End Page
- 143
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/3027
- DOI
- 10.1016/j.ijpharm.2019.02.002
- ISSN
- 0378-5173
- Abstract
- The objective of current study was to develop solid lipid nanoparticles-loaded with simvastatin (SIM-SLNs) and investigate their in vivo anti-hyperlipidemic activity in poloxamer-induced hyperlipidemia model. Nano-template engineering technique was used to prepare SIM-SLNs with palmityl alcohol as lipid core and a mixture of Tween 40/Span 40/Myrj 52 to stabilize the core. The prepared SIM-SLNs were evaluated for physicochemical parameters including particle diameter, surface charge, morphology, incorporation efficiency, thermal behaviour and crystallinity. In vitro release profile of SIM-SLNs in simulated gastric and intestinal fluids was evaluated by using dialysis bag technique and anti-hyperlipidemic activity was assessed in hyperlipidemia rat model. SIMSLNs revealed uniform particle size with spherical morphology, zeta potential of -24.9 mV and high incorporation efficiency (similar to 85%). Thermal behaviour and crystallinity studies demonstrated successful incorporation of SIM in the lipid core and its conversion to amorphous form. SIM-SLNs demonstrated a sustained SIM release from the lipid core of nanoparticles. SIM-SLNs significantly reduced the elevated serum lipids as indicated by similar to 3.9 and similar to 1.5-times decreased total cholesterol compared to those of untreated control and SIM dispersion treated hyperlipidemic rats. In conclusion, SIM-SLNs showed a great promise for improving the therapeutic outcomes of SIM via its effective oral delivery.
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