D-Optimal Mixture Design Enabled Development of Lyophilized Nanoemulsifying Drug Delivery System of Paliperidone

Title:D-Optimal Mixture Design Enabled Development of Lyophilized Nanoemulsifying Drug Delivery System of Paliperidone

Volume: 14 Issue: 2

Author(s): Prativa Das*, Jyanaranjan Panda, Kahnu Charan Panigrahi, Chinam Niranjan Patra and Goutam Kumar Jena

Affiliation:

• Department of Pharmaceutics, Roland Institute of Pharmaceutical Sciences, Berhampur, Affiliated to the Biju Patnaik University of Technology, Odisha, India

Keywords: NEDDS, mean globule size, bioavailability, stability study, lyophilized, paliperidone.

Abstract:

Background: Schizophrenia is a chronic disease with acute psychotic symptoms, which is having frequent recurrence. Paliperidone palmitate (PP) is a second-generation antipsychotic drug to treat schizophrenia.

Aims: The aim of the study was to prepare lyophilized nanoemulsifying drug delivery system (NEDDS) of paliperidone (PD).

Objective: The primary objective of the current research work was to develop a lyophilized nanoemulsifying drug delivery system (NEDDS) of paliperidone (PD) to improve its oral bioavailability and stability.

Methods: Optimization using D-Optimal Mixture Design DMD) was conducted, and optimized NEDDS was further lyophilized to improve stability. The lyophilized optimized NEDDS was further evaluated for biopharmaceutical evaluation.

Result: A saturation solubility study revealed Peceol, Tween 80, and Plurol Olique CC497 as suitable candidates for oil, surfactant, and co-surfactant, respectively. Optimized NEDDS of PD showed mean globule size (MGS) of 185 nm, PDI of 0.27 and cumulative % drug release within 15 min Q15 of 86.6%. Lyophilized optimized NEDDS was found to have no significant change in quality attributes within the stability study period. A pharmacokinetic study revealed more than two-fold increases in bioavailability for lyophilized optimized NEDDS.

Conclusion: Hence, lyophilized NEDDS of PD can be used as an effective approach for the improvement of oral bioavailability and stability.

Cite this article as:

Das Prativa*, Panda Jyanaranjan, Panigrahi Charan Kahnu, Patra Niranjan Chinam and Jena Kumar Goutam, D-Optimal Mixture Design Enabled Development of Lyophilized Nanoemulsifying Drug Delivery System of Paliperidone, Drug Delivery Letters 2024; 14 (2) . https://dx.doi.org/10.2174/0122103031273803231221070539