NDLI: Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

Content Provider	Springer Nature Link
Author	Lopes de Araújo, José Neves, Ana Rute Gouveia, Virgínia M. Moura, Catarina C. Nunes, Cláudia Reis, Salette
Copyright Year	2015
Abstract	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.Two formulations containing oxaprozin were developed: NLCs with and without folate functionalization. In order to target the macrophages folate receptors, a DSPE-PEG$_{2000}$-FA conjugate was synthesized and added to the NLCs.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.The developed nanoparticles enclose a great potential for oxaprozin oral administration with significant less gastric side-effects.
Starting Page	301
Ending Page	314
Page Count	14
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	33
Issue Number	2
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2015-09-09
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

Structural Characterization of Q10-Loaded Solid Lipid Nanoparticles by NMR Spectroscopy

Controlled Nucleation of Lipid Nanoparticles

Inhalable Microparticles as Carriers for Pulmonary Delivery of Thymopentin-Loaded Solid Lipid Nanoparticles

Overcoming Glucocorticoid Resistances and Improving Antitumor Therapies: Lipid and Polymers Carriers

Lipid Nanoparticles Loaded with an Antisense Oligonucleotide Gapmer Against Bcl-2 for Treatment of Lung Cancer

Physicochemical Investigations on Solid Lipid Nanoparticles and on Oil-Loaded Solid Lipid Nanoparticles: A Nuclear Magnetic Resonance and Electron Spin Resonance Study

Magnetic Nanoparticles for Biomedical Applications

Inhibition of HIV-1 in Cell Culture by Oligonucleotide-Loaded Nanoparticles

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

Similar Documents

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

Structural Characterization of Q10-Loaded Solid Lipid Nanoparticles by NMR Spectroscopy

Controlled Nucleation of Lipid Nanoparticles

Inhalable Microparticles as Carriers for Pulmonary Delivery of Thymopentin-Loaded Solid Lipid Nanoparticles

Overcoming Glucocorticoid Resistances and Improving Antitumor Therapies: Lipid and Polymers Carriers

Lipid Nanoparticles Loaded with an Antisense Oligonucleotide Gapmer Against Bcl-2 for Treatment of Lung Cancer

Physicochemical Investigations on Solid Lipid Nanoparticles and on Oil-Loaded Solid Lipid Nanoparticles: A Nuclear Magnetic Resonance and Electron Spin Resonance Study

Magnetic Nanoparticles for Biomedical Applications

Inhibition of HIV-1 in Cell Culture by Oligonucleotide-Loaded Nanoparticles

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects