Title:In-vitro Lipolysis, Stability and Pharmacodynamic Study of Cilnidipine Loaded Self-emulsifying Drug Delivery System
Volume: 20
Issue: 2
Author(s): Renu Kadian and Arun Nanda*
Affiliation:
- Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, India
Keywords:
Cilnidipine, in vitro lipolysis, stability, pharmacodynamic, self-emulsifying drug delivery system, ICH guidelines.
Abstract:
Aims: The aim of this research work was to investigate the potential ability of cilnidipine-
loaded-Self-Emulsifying Drug Delivery System (SEDDS) to improve the solubility and oral
bioavailability of cilnidipine.
Background: The therapeutic value of drugs is constrained by the low oral bioavailability of BCS
class II drugs. In order to improve the solubility and oral bioavailability of poorly water-soluble
drugs, SEDDS are frequently utilised.
Methods: To develop the cilnidipine-loaded-SEDDS formulation, Canola oil as the oil phase, tween
80 as the surfactant, and PEG 300 as the co-surfactant were used. The SEDDS formulation was
evaluated based on stability study per ICH guidelines, drug precipitation during in-vitro lipolysis
study under fasted and fed state, and in vivo pharmacodynamic study in Wistar rats. The content of
the drug was determined by assay of SEDDS formulation using the official method of cilnidipine.
Results: The pharmacodynamic study demonstrated that cilnidipine-loaded SEDDS formulation
significantly produced a rapid antihypertensive effect (within 2 h) that lasted for 24 h in comparison
to drug suspension. During the in vitro lipolysis study, the concentration of the drug recovered from
the aqueous phase under both fasted and fed state was more than 90% after 10 minutes, with a minute
amount of drug involved in precipitation. At stability conditions of 30 ± 2°C/65 ± 5%RH for a
duration of six months, the SEDDS formulation was found to be stable. The content of cilnidipine
in the SEDDS formulation was found to be 98.4%.
Conclusion: A BCS class-II drug's oral bioavailability and dissolution might be improved using the
self-emulsifying drug delivery method.
