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Drug Delivery Letters

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ISSN (Print): 2210-3031
ISSN (Online): 2210-304X

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Research Article

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

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

Volume 14, Issue 2, 2024

Published on: 24 January, 2024

Page: [165 - 178] Pages: 14

DOI: 10.2174/0122103031273803231221070539

Price: $65

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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).

Objectives: 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.

Results: 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.

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

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