Development and characterization of paliperidone loaded nanostructured lipid carrier
By: Dash, Sanat Kumar
.
Contributor(s): Patra, Chinam Niranjan.
Publisher: Bangalore Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(4), Oct-Dec.Description: 1003-1012p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical education and researchSummary: Background: Paliperidone is indicated for the treatment of schizophrenia. It has an absolute
oral bioavailability of about 28% as it is poorly soluble in water and also undergoes
hepatic first-pass metabolism. Objectives: The purpose of the present study is to improve
the solubility,
in vitro bioavailability of paliperidone by formulating nanostructured lipid
carrier (NLC). Materials and Methods: High shear homogenization followed by the ultra-
sonication technique was used for the preparation of NLCs loaded with Paliperidone, and
were prepared by varying weight of solid and liquid lipid in different ratios. Lyophilization
of the selected NLC was carried out to further improve its stability. Results: Glyceryl
monostearate, Linoleic acid, and Tween 80 to Tween 20 (2:1) were selected as solid
lipid, liquid lipid, and surfactant correspondingly for the development of NLC. NLC
formulation F5 was selected as the best formulation as it exhibited lowest particle size,
PDI with stable zeta potential and drug release for 12 hr. Selected NLC F5 was further
lyophilized to improve the stability using different cryoprotectants
vis-à-vis sucrose,
sorbitol and aerosol. Lyophilized NLC showed a slight increase in particle size. DSC and
P-XRD study revealed molecular dispersion of paliperidone in lipid matrix. Conclusion:
Hence the approach of formulating lyophilized NLC for paliperidone has the potential of
improving
in-vitro bioavailability.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2023-0096 |
Background: Paliperidone is indicated for the treatment of schizophrenia. It has an absolute
oral bioavailability of about 28% as it is poorly soluble in water and also undergoes
hepatic first-pass metabolism. Objectives: The purpose of the present study is to improve
the solubility,
in vitro bioavailability of paliperidone by formulating nanostructured lipid
carrier (NLC). Materials and Methods: High shear homogenization followed by the ultra-
sonication technique was used for the preparation of NLCs loaded with Paliperidone, and
were prepared by varying weight of solid and liquid lipid in different ratios. Lyophilization
of the selected NLC was carried out to further improve its stability. Results: Glyceryl
monostearate, Linoleic acid, and Tween 80 to Tween 20 (2:1) were selected as solid
lipid, liquid lipid, and surfactant correspondingly for the development of NLC. NLC
formulation F5 was selected as the best formulation as it exhibited lowest particle size,
PDI with stable zeta potential and drug release for 12 hr. Selected NLC F5 was further
lyophilized to improve the stability using different cryoprotectants
vis-à-vis sucrose,
sorbitol and aerosol. Lyophilized NLC showed a slight increase in particle size. DSC and
P-XRD study revealed molecular dispersion of paliperidone in lipid matrix. Conclusion:
Hence the approach of formulating lyophilized NLC for paliperidone has the potential of
improving
in-vitro bioavailability.
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