Nanomedicines for ocular NSAIDs: safety on drug delivery

Araújo, Joana; González‐Mira, Elisabet; Egea, M.A.; García, Montse; Souto, Eliana B.

doi:10.1016/j.nano.2009.02.003

Cited by 204 publications

(126 citation statements)

References 67 publications

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“…The approach of using a cationic lipid is interesting since ocular mucosa depicts slightly negative charge above its isoelectric point and also could improve some limitations related to ocular administration, such as prevent tear washout (due to tear dynamics), increase ocular bioavailability and prolong the residence time of drugs in the cul-de-sac (Araujo et al, 2009).…”

Section: Resultsmentioning

confidence: 99%

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Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Fangueiro

Andreani

Egea

et al. 2014

International Journal of Pharmaceutics

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127

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a b s t r a c tIn the present study we have developed lipid nanoparticle (LN) dispersions based on a multiple emulsion technique for encapsulation of hydrophilic drugs or/and proteins by a full factorial design. In order to increase ocular retention time and mucoadhesion by electrostatic attraction, a cationic lipid, namely cetyltrimethylammonium bromide (CTAB), was added in the lipid matrix of the optimal LN dispersion obtained from the factorial design. There are a limited number of studies reporting the ideal concentration of cationic agents in LN for drug delivery. This paper suggests that the choice of the concentration of a cationic agent is critical when formulating a safe and stable LN. CTAB was included in the lipid matrix of LN, testing four different concentrations (0.25%, 0.5%, 0.75%, or 1.0%wt) and how composition affects LN behavior regarding physical and chemical parameters, lipid crystallization and polymorphism, and stability of dispersion during storage. In order to develop a safe and compatible system for ocular delivery, CTAB-LN dispersions were exposed to Human retinoblastoma cell line Y-79. The toxicity testing of the CTAB-LN dispersions was a fundamental tool to find the best CTAB concentration for development of these cationic LN, which was found to be 0.5 wt% of CTAB.

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Section: Resultsmentioning

confidence: 99%

“…In addition, it is known that the smaller the particle size, the longer the retention time and easier application (Araujo et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Fangueiro

Andreani

Egea

et al. 2014

International Journal of Pharmaceutics

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127

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“…NSAIDs are a very heterogeneous group of molecules with different molecular structures, being the majority organic acids with low water solubility [18,30,[32][33][34]. NSAIDs capability to interact with COX-1 and COX-2 is directly related to its chemical properties allowing the carboxylic acid the interaction with COX-1 and having lipophilic drugs a more strong interaction with COX-2 [35].…”

Section: Chemical Classificationmentioning

confidence: 99%

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

et al. 2015

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“…The cornea is a significant mechanical and chemical obstacle and its main task is the safeguard of the intraocular tissues of the eye. The cornea is depicted by lipophilic and hydrophilic structures and reflects an effectual obstacle to the absorption of both hydrophilic and lipophilic molecules (2,3). Because of the tightness of the corneal barrier and quick loss of the instilled drug solution from the precorneal area, the bioavailability lessens.…”

Section: Introductionmentioning

confidence: 99%

A Novel Microemulsion System for Ocular Delivery of Azithromycin: Design, Characterization and Ex-Vivo Rabbit Corneal Permeability

Salimi

Panahi-Bazaz

2017

Jundishapur J Nat Pharm Prod

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Background: The poor bioavailability of ophthalmic drops is mainly due to the rapid nasolacrimal drainage of the drug and very low permeability of corneal epithelium. Hence, there is an interest to find an effective system to improve drug permeability and bioavailability. Objectives: The aim of the present study was to design and characterize a novel microemulsion system as an ocular delivery system for Azithromycin and evaluate its physicochemical characteristics and rabbit corneal permeability in order to enhance the penetration of the drug. Methods: The prepared microemulsions (MEs) were assessed for their viscosity, pH, particle size, surface tension, DSC, stability, in vitro drug release, and corneal rabbit permeability. In this study, a full factorial design was employed with 3 variables at 2 levels for preparing 8 formulations and data analysis. Results:The results showed that the average droplet size of ME formulations was in the range of 6.78 to 26.65 nm while pH values were 5.1 to 5.7 and viscosity range was 115 -361 cps. Drug release profile revealed that 79.066% of the drug released in 24 hours of the experiment. The maximum and minimum percentages of drug permeated through rabbit cornea were observed in MEA-7 (12.87%) and MEA-2 (0.909%), respectively. All ME formulations with different compositions and properties significantly increased partitioning, flux, and permeability coefficient from rabbit cornea. Dapp and Papp parameters in MEA-1 and MEA-7 formulations were 0.00882 cm 2 h -1 and 2.391 cmh -1 , which were 17.65, 35.17 times higher than those of control (AZ suspension, 1%), respectively. The

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Nanomedicines for ocular NSAIDs: safety on drug delivery

Cited by 204 publications

References 67 publications

Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

A Novel Microemulsion System for Ocular Delivery of Azithromycin: Design, Characterization and Ex-Vivo Rabbit Corneal Permeability

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