Development of acetazolamide-loaded, pH-triggered polymeric nanoparticulate<i>in situ</i>gel for sustained ocular delivery:<i>in vitro. ex vivo</i>evaluation and pharmacodynamic study

Singh, Jaskaran; Chhabra, Gulshan; Pathak, Kamla

doi:10.3109/03639045.2013.814061

Cited by 69 publications

(27 citation statements)

References 41 publications

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“…This might led to several problems in handling, manufacturing, and administration. At higher values of more than 37 °C, gel would not form at the temperature of ocular cavity so result in rapid ocular clearance of administered drug because it remain in sol form (27). When temperature is increased, the number of vesicles formed increases due to negative coefficient of solubility of niosomes.…”

Section: Discussionmentioning

confidence: 99%

Exploring the potential of complex-vesicle based niosomal ocular system loaded with azithromycin: Development of in situ gel and ex vivo characterization

2017

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Section: Discussionmentioning

confidence: 99%

Exploring the potential of complex-vesicle based niosomal ocular system loaded with azithromycin: Development of in situ gel and ex vivo characterization

2017

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“…37 Ps, ZP, and morphology of PUe-scU clNs Appropriate PS and a narrow size range in the ophthalmic formulation can ensure low irritation, sufficient bioavailability, and good compatibility in ocular tissues. 38 Therefore, the PS of the ophthalmic formulation has a significant effect on ophthalmic preparations. The mean diameter of the PUE-SCU CLNs was 181.0 nm with a PI of 0.224 (Figure 2A).…”

Section: Results and Discussion Central Ccdmentioning

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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“…Nanoparticles on a scale of 10-1000 nm offer a unique platform for drug delivery. Recent in-vivo studies of nanoparticle-based delivery of carbonic anhydrase inhibitors [13][14][15][16], brimonidine [17] and pilocarpine [18] have demonstrated superior drug stability and corneal permeation than commercial solutions. Jain et al [11] studied a nanoparticle-based system containing betaxolol hydrochloride in a dexamethasone-induced glaucoma rabbit model.…”

Section: Nanoparticle-based Topical Formulationsmentioning

confidence: 99%

Sustained drug delivery in glaucoma

Knight

Lawrence

2014

Current Opinion in Ophthalmology

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Novel platforms for providing sustained drug delivery in glaucoma continue to evolve. The ability to incorporate effective commercially available drugs into more stable compounds is an important element. Although more research is needed to establish their clinical efficacy, novel delivery systems will allow for more targeted medical therapy and for the opportunity to further explore neuroprotective and gene-based therapies.

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Development of acetazolamide-loaded, pH-triggered polymeric nanoparticulatein situgel for sustained ocular delivery:in vitro. ex vivoevaluation and pharmacodynamic study

Cited by 69 publications

References 41 publications

Exploring the potential of complex-vesicle based niosomal ocular system loaded with azithromycin: Development of in situ gel and ex vivo characterization

Exploring the potential of complex-vesicle based niosomal ocular system loaded with azithromycin: Development of in situ gel and ex vivo characterization

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

Sustained drug delivery in glaucoma

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