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Oxaprozin-Loaded Lipid Nanoparticles Towards Overcoming NSAIDs Side-Effects

Oxaprozin-Loaded Lipid Nanoparticles Towards Overcoming NSAIDs Side-Effects

José Lopes-de-Araújo, Ana Rute Neves, Virgínia M Gouveia, Catarina C Moura, Cláudia Nunes, Salette Reis

Pharm Res. 2016 Feb;33(2):301-14.

PMID: 26350105

Abstract:

Purpose:
Nanostructured Lipid Carriers (NLCs) loading oxaprozin were developed to address an effective drug packaging and targeted delivery, improving the drug pharmacokinetics and pharmacodynamics properties and avoiding the local gastric side-effects. Macrophages actively phagocyte particles with sizes larger than 200 nm and, when activated, over-express folate beta receptors - features that in the case of this work constitute the basis for passive and active targeting strategies.
Methods:
Two formulations containing oxaprozin were developed: NLCs with and without folate functionalization. In order to target the macrophages folate receptors, a DSPE-PEG2000-FA conjugate was synthesized and added to the NLCs.
Results:
These formulations presented a relatively low polydispersity index (approximately 0.2) with mean diameters greater than 200 nm and zeta potential inferior to -40 mV. The encapsulation efficiency of the particles was superior to 95% and the loading capacity was of 9%, approximately. The formulations retained the oxaprozin release in simulated gastric fluid (only around 10%) promoting its release on simulated intestinal fluid. MTT and LDH assays revealed that the formulations only presented cytotoxicity in Caco-2 cells for oxaprozin concentrations superior to 100 μM. Permeability studies in Caco-2 cells shown that oxaprozin encapsulation did not interfered with oxaprozin permeability (around 0.8 × 10(-5) cm/s in simulated intestinal fluid and about 1.45 × 10(-5) cm/s in PBS). Moreover, in RAW 264.7 cells NLCs functionalization promoted an increased uptake over time mainly mediated by a caveolae uptake mechanism.
Conclusions:
The developed nanoparticles enclose a great potential for oxaprozin oral administration with significant less gastric side-effects.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP21256188-A	Oxaprozin		21256-18-8	Price

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