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

1. Pak J Pharm Sci. 2026 Oct 1;39(10):3186-3196. doi: 10.36721/PJPS.2026.39.10.295.1. Formulation and evaluation of sustained-release pitavastatin-loaded chitosan nanoparticles for enhanced anti-hyperlipidemic activity. Arshad A(1), Zaman M(2), Riaz H(1), Haider MS(3), Ishaq W(4), Adnan S(5), Masood Z(3), Ahmed H(6), Ameer N(3), Rahman HMA(7), Waqas M(8), Farooq M(3). Author information: (1)Rashid Latif College of Pharmacy, Lahore, Pakistan. (2)Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan. (3)School of Pharmacy, Multan University of Science and Technology, Multan, Pakistan. (4)Faculty of Pharmacy, The University of Lahore, Lahore, Pakistan. (5)Allied Institute, Multan, Pakistan. (6)Sialkot Institute of Science and Technology, Sialkot, Pakistan. (7)Southern Punjab Institute of Health Sciences, Multan, Pakistan. (8)School of Computing, Engineering and the Built Environment, Edinburgh Napier University, Edinburgh, EH10 5DT, UK. 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. DOI: 10.36721/PJPS.2026.39.10.295.1 PMID: 42489300 [Indexed for MEDLINE]

{
  "language": "lang-en",
  "diagnosis": [
    "ra"
  ],
  "specialty": "rheumatology",
  "study_type": "cohort",
  "evidence_level": "level-3",
  "v6_autopublish": true,
  "clinical_impact": "moderate-impact",
  "practice_recommendation": "monitoring"
}