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Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity.

Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity.

期刊: Pakistan journal of pharmaceutical sciences 日期: 2026-10-01 PMID: 42489300 DOI: 10.36721/PJPS.2026.39.10.295.1 浏览: 19
作者: Arshad A, Zaman M, Riaz H, Haider MS, Ishaq W, Adnan S, Masood Z, Ahmed H, Ameer N, Rahman HMA
A, A., M, Z., H, R., MS, H., W, I., S, A., Z, M., H, A., N, A., & HMA, R. (2026). Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity.. Pakistan journal of pharmaceutical sciences. https://doi.org/10.36721/PJPS.2026.39.10.295.1
A A, M Z, H R, MS H, W I, S A, et al. Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity.. Pakistan journal of pharmaceutical sciences. 2026; doi: 10.36721/PJPS.2026.39.10.295.1
A A, M Z, H R, et al. Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity.[J]. Pakistan journal of pharmaceutical sciences. 2026. DOI: 10.36721/PJPS.2026.39.10.295.1.
@article{a2026,
  author = {Arshad A and Zaman M and Riaz H and Haider MS and Ishaq W and Adnan S and Masood Z and Ahmed H and Ameer N and Rahman HMA},
  title = {Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity.},
  journal = {Pakistan journal of pharmaceutical sciences},
  year = {2026},
  doi = {10.36721/PJPS.2026.39.10.295.1},
  note = {PMID: 42489300},
}
TY  - JOUR
AU  - Arshad A
AU  - Zaman M
AU  - Riaz H
AU  - Haider MS
AU  - Ishaq W
AU  - Adnan S
AU  - Masood Z
AU  - Ahmed H
AU  - Ameer N
AU  - Rahman HMA
TI  - Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity.
T2  - Pakistan journal of pharmaceutical sciences
PY  - 2026
DO  - 10.36721/PJPS.2026.39.10.295.1
AN  - PMID:42489300
ER  - 

摘要

BACKGROUND: Pitavastatin (PVN), a BCS class-II drug, exhibits poor aqueous solubility leading to limited oral bioavailability and therapeutic efficacy. OBJECTIVES: This study aimed to enhance the solubility and anti-hyperlipidemic efficacy of Pitavastatin (PVN) by encapsulating it in chitosan-based polymeric nanoparticles. METHODS: Pitavastatin-loaded chitosan nanoparticles (NPs) were prepared using the ionic gelation method. Formulations were characterized by particle size, zeta potential, drug loading, In-vitro drug release and surface morphology. Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), thermal analysis (TGA and DSC), ex-vivo intestinal permeability and in-vivo pharmacodynamic analysis were also performed. RESULTS: The size of PVN-loaded NP ranged from 219.9±1.11 to 292.7±2.29 nm with PDI 0.2-0.4, surface charge of +28.4 ± 0.43 to 32.5 ± 1.02 mV and entrapment efficiency 65±1.12-93±1.23%. Solubility in different media (PBS (pH 6.8), 0.1N HCl (pH 1.2) and distilled water showed a 56-102-fold increase compared to PVN. SEM analysis revealed a smooth surface and spherical geometry of the NP. FTIR analysis confirmed that there was no physicochemical interaction between PVN and chitosan in NP formulations (NP1-NP5). XRD and thermal analysis indicated the amorphous nature of PVN-loaded NP. In-vitro drug release from NP formulations (NPI-NP5) ranged from 80.97±4.80 to 81±3.90% indicating sustained release, while ex-vivo intestinal permeability was 1.5-fold higher than PVN. The optimized formulation (NP1) followed Higuchi release model, indicating Fickian diffusion. Pharmacodynamic analysis of lipid profiles in hyperlipidemic albino rats suggested that NP1 reduced low-density lipoprotein (LDL) by 33±1.24 %, total cholesterol by 29±2.13% and triglycerides by 23±1.21%, showing better results than PVN. CONCLUSION: Chitosan-based Pitavastatin nanoparticles successfully enhanced drug solubility and provided sustained release, leading to improved ex-vivo permeability and greater in-vivo anti-hyperlipidemic activity in albino rats. This approach represents a promising strategy for enhancing therapeutic potential of Pitavastatin.

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