Recent advances in topical ophthalmic drug delivery with lipid-based nanocarriers

Gan, Li; Wang, Jing; Jiang, Min; Bartlett, Hanah; Ouyang, Defang; Eperjesi, Frank; Liu, Jianping; Gan, Yong

doi:10.1016/j.drudis.2012.10.005

Cited by 219 publications

(122 citation statements)

References 60 publications

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“…These nanocarriers may be in the form of liposomes [5], cubosomes, niosomes, cyclodextrins, dendrimers, micelles, solid lipid nanoparticles, core shell nanoassemblies and silica particles [6]. Lipid components of the nanocarrier may interact with the lipid part of tear drop thereby enabling the drug to stay in the conjunctival area for an increased time where they may perform as drug storehouse [7–9]. …”

Section: Introductionmentioning

confidence: 99%

Impediment of selenite-induced cataract in rats by combinatorial drug laden liposomal preparation

Huang

Muhemaitia

2018

Libyan Journal of Medicine

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Cataract is the leading cause of blindness globally with surgery being the only form of treatment. But cataract surgery is accompanied by complications, chiefly intra-ocular infections. Hence, preventive nanoformulations may be extremely beneficial. In the present study, novel chitosan-coated liposomal formulations encapsulating a combination of drugs, lanosterol and hesperetin were prepared and characterized. The combinatorial liposomes were prepared by thin film evaporation active extrusion method. The characterization of liposomes was done by transmission electron microscopy, zeta potential, encapsulation efficiency, stability, cytotoxicity and in vitro release studies. The main difference between the chitosan-coated and uncoated combinatorial liposomes is the release of drugs as indicated by the in vitro release studies. The slow and sustained release of the drugs from chitosan-coated ones as against the burst release from uncoated indicates an increased retention time for combinatorial drugs in cornea. This leads to a delay in progression of cataract as seen from in vivo studies. Cytotoxicity studies indicate no cell toxicity of the coating of chitosan or the combination of drugs. Stability studies indicate that there were almost no changes in size, zeta potential and polydispersity index values of the combinatorial liposomes upon storage at room temperature for 60 days. Another important study is the estimation of antioxidant defense system. The estimated values of glutathione reductase, malondialdehyde and chief antioxidant enzymes point toward an upregulation of antioxidant defense system. From the results, it may be concluded that novel chitosan-coated combinatorial liposomes are effective in delaying or preventing of cataract.

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Section: Introductionmentioning

confidence: 99%

Impediment of selenite-induced cataract in rats by combinatorial drug laden liposomal preparation

Huang

Muhemaitia

2018

Libyan Journal of Medicine

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“…These conventional dosage forms account for nearly 90% of the currently available marketed formulations due to their simplicity, safety, and acceptance by patients. 5 However, the physiological constraints imposed by the protective mechanisms of the eye and the limited permeability of the cornea lead to low absorption of ocular drugs and result in a short therapeutic effect. 6 In addition, drugs exit the tear volume as tear fluid, which is continuously drained from the eyes to the nose during blinking, resulting in reduced bioavailability.…”

Section: Introductionmentioning

confidence: 99%

“…43 One potential mechanism for enhancing corneal permeation was cationic material modification of lipid-based nanoparticles, which has been found to improve spreading properties, reduce contact angles, and increase residence time on the ocular surface, possibly interacting with the lipid layer of the tear film, so that the carrier can be retained in the conjunctival sac for a long period, where it acts as a drug depot. 5,44 Another potential mechanism was that the liquid nanoparticles possess a bioadhesive property due to extremely small PS and increased surface area, which could promote permeation of the drug. Moreover, Gelucire ® 44/14 has been reported to be an effective corneal permeation enhancer.…”

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confidence: 99%

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Wang¹,

Zhao²,

Li³

et al. 2017

IJN

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The purpose of this study was to prepare, optimize, and characterize a cationic lipid nanoparticle (CLN) system containing multicomponent drugs using a molecular dynamics model as a novel method of evaluating formulations. Puerarin (PUE) and scutellarin (SCU) were used as model drugs. CLNs were successfully prepared using melt-emulsion ultrasonication and low temperature-solidification technique. The properties of CLNs such as morphology, particle size, zeta potential, entrapment efficiency (EE), drug loading (DL), and drug release behavior were investigated. The CLNs were evaluated by corneal permeation, preocular retention time, and pharmacokinetics in the aqueous humor. Additionally, a molecular dynamics model was used to evaluate the formulation. Electron microscopy results showed that the nanoparticles were approximately spherical in shape. The EE (%) and DL (%) values of PUE and SCU in the optimal formulation were 56.60±3.73, 72.31±1.96 and 1.68±0.17, 2.44±1.14, respectively. The pharmacokinetic study in the aqueous humor showed that compared with the PUE and SCU solution, the area under the concentration–time curve (AUC) value of PUE was enhanced by 2.33-fold for PUE-SCU CLNs ( p <0.01), and the SCU AUC was enhanced by 2.32-fold ( p <0.01). In the molecular dynamics model, PUE and SCU passed through the POPC bilayer, with an obvious difference in the free energy well depth. It was found that the maximum free energy required for PUE and SCU transmembrane movement was ~15 and 88 kJ·mol −1 , respectively. These findings indicated that compared with SCU, PUE easily passed through the membrane. The diffusion coefficient for PUE and SCU were 4.1×10 −3 ±0.0027 and 1.0×10 −3 ±0.0006 e −5 cm 2 ·s −1 , respectively. Data from the molecular dynamics model were consistent with the experimental data. All data indicated that CLNs have a great potential for ocular administration and can be used as an ocular delivery system for multicomponent drugs. Moreover, the molecular dynamics model can also be used as a novel method for evaluating formulations.

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“…Cyclosporine A and latanoprost cationic emulsions are currently in phase III clinical trials. Tear Again ® is a liposomal spray for dry eye syndrome [17]. Durasite ® DDS polycarbophil based aqueous solution with innate ability for hydrogen-bonding with the mucus, corneal and conjunctival epitheliums, to provide the sustained effect [18,19].…”

Section: Literature Review Novel Drug Delivery Systemsmentioning

confidence: 99%

Emerging Trends in Ocular Drug Delivery: A Review on Recent Updates

Imtiazul¹,

Auniq²

2017

J Neoplasm

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The distance from cornea to retina (1.7 cm) appears to be the difficult path for most of the small molecule therapeutics. Ocular drug delivery is extreme difficult task owing to complexity and intricate barriers of the eye. However, there is an urgency and need to overcome these barriers for the treatment of sight threatening ocular complications. Delivery of drugs through topical application is compromised by physiological, static, dynamic and metabolic barriers. Currently, intravitreal therapy is a gold standard for targeting therapeutic entities to the posterior segment of the eye. Various viable platforms using topical non-invasive to invasive techniques are currently under development and may progress into efficient delivery platforms. In this review, recent advances/developments in ocular delivery were discussed.

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Recent advances in topical ophthalmic drug delivery with lipid-based nanocarriers

Cited by 219 publications

References 60 publications

Impediment of selenite-induced cataract in rats by combinatorial drug laden liposomal preparation

Impediment of selenite-induced cataract in rats by combinatorial drug laden liposomal preparation

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Emerging Trends in Ocular Drug Delivery: A Review on Recent Updates

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