DEVELOPMENT, OPTIMIZATION AND IN VITRO CHARACTERIZATION OF HALOPERIDOL NANOCRYSTALS USING 32 FACTORIAL DESIGN

DAMINENI SARITHA; P. SUBHASH CHANDRA BOSE; RIYAZ ALI M. OSMANI; PADMINI IRIVENTI; SANDEEP KANNA; GUNDAWAR RAVI

doi:10.22159/ijap.2024v16i3.50412

Authors

DAMINENI SARITHA Department of Pharmaceutics, Sultan-ul-Uloom College of Pharmacy, Hyderabad-500034, Telangana State, India https://orcid.org/0000-0001-5056-8989
P. SUBHASH CHANDRA BOSE Department of Pharmaceutics, MNR College of Pharmacy, Sangareddy, Telangana State, India https://orcid.org/0000-0002-9365-0701
RIYAZ ALI M. OSMANI Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research (JSSAHER), Mysuru-570015, Karnataka, India
PADMINI IRIVENTI Department of Pharmaceutics, Smt. Sarojini Ramulamma College of Pharmacy, Mahabubnagar- 509001, Telangana, India https://orcid.org/0000-0002-7513-9803
SANDEEP KANNA Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Guntur - 522034, Andhra Pradesh, India https://orcid.org/0000-0002-1524-6068
GUNDAWAR RAVI Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal-576104, Karnataka, India https://orcid.org/0000-0002-4041-0560

DOI:

https://doi.org/10.22159/ijap.2024v16i3.50412

Keywords:

Haloperidol, Antipsychotic drug, BCS- II class of drugs, 32 factorial design

Abstract

Objective: The main aim of the present study was to improve the dissolution rate of Haloperidol nanocrystals and thereby increase their bioavailability. Haloperidol is a typical antipsychotic drug and it is used to treat schizophrenia as well as acute mania and mixed states associated with bipolar disorder. Haloperidol falls into the Biopharmaceutics Classification System (BCS- II) class of drugs (poorly soluble aqueous and highly permeable) and has poor bioavailability.

Methods: The present study involves the preparation and optimization of Haloperidol nanocrystals by the anti-solvent precipitation method using Polaxomer407 and polyvinyl pyrrolidone K30 (PVP K30). The prepared nanocrystals were evaluated for various parameters like particle size, zeta potential, % drug content, % yield, surface morphology, drug-excipient compatibility studies (Fourier-transform infrared spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC)), and in-vitro dissolution studies.

Results: Nine preparations were done and the best preparation amongst them was selected for further studies. F₇preparation containingpolaxomer407 and PVP K30 was selected as optimized preparation based on their evaluation parameters. 3² factorial design was used in the preparation. The particle size of the F₇ nanocrystals was 300.2±2.7 nm and the zeta potential -36.3±3.2 mV. The % yield was in the range of 63.62±0.3% -98.21±0.8 %. The drug content of various preparations was found to be in the range of 58.46±0.8% -93.54±0.5 %. In-vitro dissolution studies showed the highest % drug release for F₇(91.54±0.03%) in 10 hrs.

Conclusion: F₇ preparation was found to be having acceptable characteristics and thus selected as optimized preparation.

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