Research ArticlesPLGA nanospheres for the ocular delivery of flurbiprofen: Drug release and interactions
Section snippets
INTRODUCTION
Significant efforts have been made over the last few decades to develop new drug delivery systems that improve the ocular administration of drugs. The use of colloidal drug delivery systems, for example, nanoparticles, is considered nowadays as a strategy that can enhance the ocular bioavailability of topically administered drugs.1 Treatment with these systems increases bioavailability, reduces administration frequency and promotes drug targeting to specific sites. Although a number of polymers
Materials
The poly(lactic-co-glycolic) acid or PLGA polymer chosen was Resomer® RG 756 (Ingelheim, Germany) with a molecular weight of 98,000 Da and a lactide/glycolide molar ratio of 75/25. Poloxamer 188 (Lutrol® F68) was obtained from BASF (Barcelona, Spain). Flurbiprofen and Ocuflur™ were obtained from Sigma (St. Louis, MO) and Allergan (Madrid, Spain), respectively. Double-distilled water was used after filtration in a Millipore® system. All other chemicals and reagents used in the study were of
Nanospheres Characterization
Table 1 describes the physicochemical parameters of the empty and optimized FB-loaded PLGA NEs (F1) obtained in our previous studies13 and the new developed formulations of FB loaded NEs (F2 and F3) prepared at the same concentration as the commercial eye drops (Ocuflur™) to perform the in vitro release and ex vivo permeation studies.
All formulations showed a mean particle size of 200–300 nm which is appropriate for ophthalmic application.21 The particle size distribution was very narrow in all
CONCLUSIONS
This study evaluated the suitability and feasibility of PLGA NEs as an ocular FB delivery system. The size and spherical morphology of the NEs prepared was suitable for ophthalmic administration. A combination of X-ray diffractometry, infrared spectroscopy, differential scanning calorimetry and thermomicroscopy showed the potential of FB-loaded NEs as a drug carrier system where drug dispersion in the polymer system increases FB solubility (FB has a plastic effect on the polymer). FB release
Acknowledgements
The authors wish to thank Hervé Rimbaud at Calytherm and Xavier Alcober in Serveis Cientificotécnics at Barcelona University for their valuable technical assistance. This work was supported by the Spanish Government (CTQ2005-09063-C03-03).
REFERENCES (39)
- et al.
Biodegradation and biocompatibility of PLA and PLGA microspheres
Adv Drug Delivery Rev
(1997) - et al.
Quantitative precorneal disposition of topically applied pilocarpine nitrate in rabbit eyes
J Pharm Sci
(1976) - et al.
Flurbiprofen-loaded acrylate polymer nanosuspensions for ophthalmic application
Biomaterials
(2002) - et al.
Flurbiprofen loaded biodegradable nanoparticles for ophthalmic administration
J Pharm Sci
(2006) - et al.
Nanocapsule formation by interfacial polymer deposition following solvent displacement
Int J Pharm
(1989) - et al.
Solid-state solubility influences encapsulation and release of hydrophobic drugs from PLGA/PLA nanoparticles
J Pharm Sci
(2004) - et al.
Flurbiprofen-loaded nanospheres: Analysis of the matrix structure by thermal methods
Int J Pharm
(1999) - et al.
Drug release from submicronized o/w emulsion: A new in vitro kinetic evaluation model
Int J Pharm
(1990) - et al.
Determination of dexamethasone in tears by capillary electrophoresis
J Chrom Biomed
(1997) - et al.
Effect of particle size on ophthalmic bioavailability of dexamethasone suspensions in rabbits
J Pharm Sci
(1980)
PLGA nanoparticles prepared by nanoprecipitation: Drug loading and release studies of a water soluble drug
J Control Release
Investigation of polymeric nanoparticles as carriers of enaprilat for oral administration
Int J Pharm
Thermoanalysis of microspheres
Thermochim Acta
Preparation, characterization and photosensivity studies of solid dispersions of diflunisal and Eudragit RS100® and RL100®
Int J Pharm
Lidocaine-loaded biodegradable nanospheres I. Optimization of the drug incorporation into the polymer Matrix
J Control Release
Lidocaine loaded biodegradable nanospheres II. Modelling of drug release
J Control Release
Study of the mechanism of interaction of poly(ε-caprolactone) nanocapsules with the cornea by confocal laser scanning microscopy
Int J Pharm
The influence of non-ionic detergents and other surfactants on human corneal permeability
Exp Eye Res
Particulates (nanoparticles and microparticles)
Cited by (130)
Sertaconazole-PLGA nanoparticles for management of ocular keratitis
2024, Journal of Drug Delivery Science and TechnologyNano-dimensional in-situ hydrogels of lifitegrast: An advancement in preservation time, sustained release and corneal healing in dry eye syndrome
2023, Journal of Drug Delivery Science and TechnologyPLGA-based nanoparticles for the treatment of inflammatory diseases
2023, Poly(lactic-co-glycolic acid) (PLGA) Nanoparticles for Drug DeliveryMolecular dynamics simulation reveals the reliability of Brij-58 nanomicellar drug delivery systems for flurbiprofen
2022, Journal of Molecular Liquids