Solid self-emulsifying casein carrier for the improvement on the oral bioavailability of simvastatin.
Int J Biol Macromol
; 268(Pt 2): 131516, 2024 May.
Article
in En
| MEDLINE
| ID: mdl-38621556
ABSTRACT
Simvastatin (SV) is a statin drug that can effectively control cholesterol and prevent cardiovascular diseases. However, SV is water-insoluble, and poor oral bioavailability (<5â¯%). Solid self-emulsifying carrier system is more stable than liquid emulsions, facilitating to improve the solubility and bioavailability of poorly soluble drugs. In the present study, a solid self-emulsifying carrier stabilized by casein (Cas-SSE) was successfully used to load SV to improve its solubility in water, by formulation selection and emulsification process optimization. Compared with oral tablets, the release of SV from Cas-SSE was significantly enhanced in artificial intestinal fluid. Furthermore, everted gut sac experiments indicated some water-soluble dispersing agents such as hydroxyethyl starch (HES), were not conducive to drug absorption. Pharmacokinetic studies suggested Cas-SSE without dispersing agent has much higher relative bioavailability (184.1â¯% of SV and 284.5â¯% of simvastatin acid) than SV tablet. The present work suggests Cas-SSE is a promising drug delivery platform with good biocompatibility for improving oral bioavailability of poorly water-soluble drugs.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Solubility
/
Drug Carriers
/
Biological Availability
/
Caseins
/
Simvastatin
/
Emulsions
Limits:
Animals
Language:
En
Journal:
Int J Biol Macromol
Year:
2024
Document type:
Article
Country of publication:
Netherlands