DOI: 10.5176/2345-783X_PHARMA17.12
Authors: Silki, V R Sinha
Abstract:
Aripiprazole is a novel and well-known for the treatment of both negative and positive symptoms associated with schizophrenia. However, aripiprazole faces a few limitations including poor aqueous solubility along with a high first pass effect that leads to low bioavailability. Purpose: Solid lipid nanoparticles (SLNs) enhance the systemic availability of the drug by virtue of their lipidic composition and nano size along with a reduction in hepatic first pass metabolism of drugs and increase in lymphatic transport of the drugs. The current work focuses on preparation and in vivo pharmacodynamic evaluation of aripiprazole loaded solid lipid nanoparticles. Methods: Aripiprazole loaded SLNs were prepared by the microemulsification method and in vitro characterization was done. Laca mice were given MK-801 i.p. at a dose of 0.5 mg/Kg for the initial five days followed by a washout period of 7 days. Treatments were given orally for 18 days starting from the 13th day of the protocol. Behavioral tests were carried out on the last four days of treatment. Animals were sacrificed on last day to collect liver and brain tissues to evaluate any signs of toxicity by histopathological studies. Results: The SLN treated groups were found to be significantly effective in reducing schizophrenic symptoms as compared to the group treated with drug suspension (p<0.05). No significant signs of toxicity were observed upon microscopic evaluation of histopathological evaluation of brain and liver tissue. Conclusion: Aripiprazole loaded SLNs were found to be significantly effective as compared to the drug suspension. The pharmacokinetic profile of prepared SLNs is being evaluated for any improvement.
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