Further investigation of nanostructured lipid carriers as an ocular delivery system: In vivo transcorneal mechanism and in vitro release study

Tian, Baocheng; Zhang, Wenji; Xu, Heming; Hao, Mei-Xia; Liu, Yun-Bin; Yang, Xinggang; Pan, Weisan; Xin-hu, Liu

doi:10.1016/j.colsurfb.2012.08.021

Cited by 46 publications

(25 citation statements)

References 15 publications

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“…NLCs consist of a mixture of solid and liquid lipids at room temperature and typically have increased drug accommodation in the solid matrix . This effect is because the mixture of solid and liquid lipids results in a greater number of imperfections in the nanoparticle crystal lattice; these imperfections leave sufficient space to accommodate the drug; thereby, the drug‐loading capacity and stability are higher over the long term relative to SLN . Both SLN and NLCs contain stabilising surfactants that form a layer of emulsifiers in aqueous dispersions …”

Section: Delivery Systemsmentioning

confidence: 99%

Topical delivery of ocular therapeutics: carrier systems and physical methods

Souza

Dias

Pereira

et al. 2014

Journal of Pharmacy and Pharmacology

117

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Objective The basic concepts, major mechanisms, technological developments and advantages of the topical application of lipid-based systems (microemulsions, nanoemulsions, liposomes and solid lipid nanoparticles), polymeric systems (hydrogels, contact lenses, polymeric nanoparticles and dendrimers) and physical methods (iontophoresis and sonophoresis) will be reviewed. Key findings Although very convenient for patients, topical administration of conventional drug formulations for the treatment of eye diseases requires high drug doses, frequent administration and rarely provides high drug bioavailability. Thus, strategies to improve the efficacy of topical treatments have been extensively investigated. In general, the majority of the successful delivery systems are present on the ocular surface over an extended period of time, and these systems typically improve drug bioavailability in the anterior chamber whereas the physical methods facilitate drug penetration over a very short period of time through ocular barriers, such as the cornea and sclera. Summary Although in the early stages, the combination of these delivery systems with physical methods would appear to be a promising tool to decrease the dose and frequency of administration; thereby, patient compliance and treatment efficacy will be improved.

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Section: Delivery Systemsmentioning

confidence: 99%

Topical delivery of ocular therapeutics: carrier systems and physical methods

Souza

Dias

Pereira

et al. 2014

Journal of Pharmacy and Pharmacology

117

View full text Add to dashboard Cite

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“…[19][20][21][22] Briefly, selected amounts of GEN (0.05%, 10 mg), Compritol 888 ATO (1.10%, 220 mg), Miglyol 812 N (0.38%, 75 mg), and Gelucire 44/14 (0.50%, 100 mg) were blended and heated under moderate stirring at 85°C to form a transparent and uniform oil phase. Then, Cremphor ® EL (1.13%, 225 mg) and EPC (0.38%, 750 mg) were dissolved in 20 mL purified water before being heated to 85°C and added dropwise to the oil phase, with magnetic stirring at 600 rpm over a period of 10 minutes.…”

Section: Preparation Of Gen-loaded Nlc (Gen-nlc)mentioning

confidence: 99%

Nanostructured lipid carrier surface modified with Eudragit RS 100 and its potential ophthalmic functions

Zhang¹,

Li²,

Ye³

et al. 2014

IJN

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This study was carried out to evaluate the ocular performance of a cationic Eudragit (EDU) RS 100-coated nanostructured lipid carrier (NLC). The genistein encapsulated NLC (GEN-NLC) was produced using the melt-emulsification technique followed by surface absorption of EDU RS 100. The EDU RS 100 increased the surface zeta potential from −7.46 mV to +13.60 mV, by uniformly forming a spherical coating outside the NLC surface, as shown by transmission electron microscopy images. The EDU RS 100 on the NLC surface effectively improved the NLC stability by inhibiting particle size growth. The obtained EDU RS 100-GEN-NLC showed extended precorneal clearance and a 1.22-fold increase in AUC (area under the curve) compared with the bare NLC in a Gamma scintigraphic evaluation. The EDU RS 100 modification also significantly increased corneal penetration producing a 3.3-fold increase in apparent permeability coefficients (P app ) compared with references. Draize and cytotoxicity testing confirmed that the developed EDU RS 100-GEN-NLC was nonirritant to ocular tissues and nontoxic to corneal cells. These results indicate that the NLC surface modified by EDU RS 100 significantly improves the NLC properties and exhibits many advantages for ocular use.

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“…Among these new delivery systems, NLC composed of a solid lipid matrix with a certain content of spatially incompatible liquid lipid appear to be the most promising candidate for ocular drug delivery 9 . NLC can improve drug bioavailability either by facilitating transcorneal penetration or by prolonging the precorneal residence time 10 . Cationic NLC (CNLC) has been recently investigated for targeting ocular mucosa, namely the posterior segment of the eye.…”

Section: Introductionmentioning

confidence: 99%