Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability

Gan, Li; Han, Shun; Shen, Junyao; Zhu, Jin; Zhu, Chunliu; Zhang, Xinxin; Gan, Yong

doi:10.1016/j.ijpharm.2010.06.015

Cited by 169 publications

(94 citation statements)

References 35 publications

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“…The region of interest (ROI) for residual fluorescence was around the ocular and non-ocular areas. 26,27 The remaining intensity (R) was calculated according to Equation 5:…”

Section: Preocular Retention Time Evaluationmentioning

confidence: 99%

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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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“…The region of interest (ROI) for residual fluorescence was around the ocular and non-ocular areas. 26,27 The remaining intensity (R) was calculated according to Equation 5:…”

Section: Preocular Retention Time Evaluationmentioning

confidence: 99%

“…26 In vivo study animals New Zealand white rabbits weighing 2.5-3.0 kg were purchased from Tianjin Yuda Experimental Animal Culture Co, Ltd, Tianjin, China. The animals were housed at 25°C±1°C and 50%±5% relative humidity with ad libitum access to food and water.…”

Section: Preocular Retention Time Evaluationmentioning

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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“…These constraints include poor corneal permeation, elimination by tears and the nasolacrimal duct, and transportation into the systemic circulation by other absorption pathways. 9 Meanwhile, both suspensions and oil solutions show poor biocompatibility and are strong irritants. Therefore, improving corneal penetration and prolonging precorneal retention time are critical aspects to be considered when designing a formulation.…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, improving corneal penetration and prolonging precorneal retention time are critical aspects to be considered when designing a formulation. Nanoscale drug delivery systems, such as nanoparticles, 10 cubosomes, 9,11 nanoemulsions, 12 and liposomes, 13 have been shown to improve corneal penetration and increase retention time. Because of their resemblance to biomembranes, liposomes have improved biocompatibility.…”

Section: Introductionmentioning

confidence: 99%

Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation

Dai¹,

Zhou²,

Liu³

et al. 2013

IJN

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Abstract:The objective of this study was to investigate the potential of liposomes containing bile salts as an ophthalmic delivery system for tacrolimus to improve corneal permeability. Liposomes containing bile salts, including sodium taurocholate, sodium deoxycholate, and sodium glycocholate, were produced by the thin-film dispersion method with a particle size of approximately 100 nm and an entrapment efficiency of more than 90%. Less than 5% tacrolimus was released from conventional liposomes and from liposomes containing sodium taurocholate, sodium deoxycholate, or sodium glycocholate over 12 hours. The cellular uptake of conventional liposomes was significantly higher than that of liposomes containing bile salts. However, liposomes containing bile salts exerted a 3-4-fold increase of tacrolimus in ex vivo corneal transport of tacrolimus compared with conventional liposomes. When rabbit eyes were treated with a DiI perchlorate-loaded liposome suspension, liposomes containing bile salts showed fast and sustained penetration across the cornea. Unfortunately, liposomes containing sodium deoxycholate caused toxicity or irritation to both spontaneously derived human corneal epithelial cells and the rabbit cornea. Therefore, liposomes containing sodium taurocholate and sodium glycocholate are potential carriers in ocular drug delivery systems, given their low toxicity and vastly improved permeability.

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“…The amount of drug loaded in the cubosome was calculated as the difference between the total amount used in preparation of the cubosome and the amount in the filtrate determined by ultraperformance liquid chromatography (UPLC). 31 The drug encapsulation efficiency was calculated as follows:…”

Section: Physicochemical Characterization Of Cubosomesmentioning

confidence: 99%

Enhanced oral absorption of 20(S)-protopanaxadiol by self-assembled liquid crystalline nanoparticles containing piperine: in vitro and in vivo studies

Jin¹,

Zhang²,

Sun³

et al. 2013

IJN

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Background: 20(S)-protopanaxadiol (PPD), similar to several other anticancer agents, has low oral absorption and is extensively metabolized. These factors limit the use of PPD for treatment of human diseases. Methods: In this study, we used cubic nanoparticles containing piperine to improve the oral bioavailability of PPD and to enhance its absorption and inhibit its metabolism. Cubic nanoparticles loaded with PPD and piperine were prepared by fragmentation of glyceryl monoolein (GMO)/poloxamer 407 bulk cubic gel and verified using transmission electron microscopy and differential scanning calorimetry. We evaluated the in vitro release of PPD from these nanoparticles and its absorption across the Caco-2 cell monolayer model, and subsequently, we examined the bioavailability and metabolism of PPD and its nanoparticles in vivo. Results: The in vitro release of PPD from these nanoparticles was less than 5% at 12 hours. PPDcubosome and PPD-cubosome loaded with piperine (molar ratio PPD/piperine, 1:3) increased the apical to basolateral permeability values of PPD across the Caco-2 cell monolayer from 53% to 64%, respectively. In addition, the results of a pharmacokinetic study in rats showed that the relative bioavailabilities of PPD-cubosome [area under concentration-time curve (AUC) 0-∞ ] and PPD-cubosome containing piperine (AUC 0-∞ ) compared to that of raw PPD (AUC 0-∞ ) were 166% and 248%, respectively. Conclusion: The increased bioavailability of PPD-cubosome loaded with piperine is due to an increase in absorption and inhibition of metabolism of PPD by cubic nanoparticles containing piperine rather than because of improved release of PPD. The cubic nanoparticles containing piperine may be a promising oral carrier for anticancer drugs with poor oral absorption and that undergo extensive metabolism by cytochrome P450.

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Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability

Cited by 169 publications

References 35 publications

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

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

Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation

Enhanced oral absorption of 20(S)-protopanaxadiol by self-assembled liquid crystalline nanoparticles containing piperine: in vitro and in vivo studies

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