Novel Nanomicellar Formulation Approaches for Anterior and Posterior Segment Ocular Drug Delivery

Cholkar, Kishore; Patel, Ashaben; Vadlapudi, Aswani Dutt; Mitra, Ashim K.

doi:10.2174/1877912311202020082

Cited by 152 publications

(83 citation statements)

References 89 publications

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“…Recently, published patents on nanotechnology-based ocular drug delivery have been discussed in various review articles. 94,95 In the current review, research articles and patents on colloidal dosage forms in the treatment of anterior chamber inflammations are discussed in the following section of this review article.…”

Section: Cyclodextrinsmentioning

confidence: 99%

“…[112][113][114][115][116][117][118][119] In a recently published review Cholkar and Mitra have discussed in detail about methods for nanomicelle preparation and their applications in ocular drug delivery. 94 Recently, Pepic et al attempted to deliver the dexamethasone-encapsulated Pluronic/chitosan micellar system. 113 It was observed that addition of chitosan to the pluronic micelle system improved in vitro drug release properties.…”

Section: Formulation Approaches For Anterior Chamber Deliverymentioning

confidence: 99%

“…In vivo studies conducted in rabbits and canines exhibited enhanced drug bioavailability to anterior segment ocular tissues with no sign of ocular irritation or toxicity. 94,120 In vivo single-dose pharmacokinetic studies with voclosporine containing nanomicellar formulation were conducted in rabbit animal models. Results demonstrated a better pharmacokinetic profile with mixed nanomicellar formulation in the anterior ocular tissues (Fig.…”

Section: Formulation Approaches For Anterior Chamber Deliverymentioning

confidence: 99%

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Novel Strategies for Anterior Segment Ocular Drug Delivery

Cholkar

Patel

Vadlapudi

et al. 2013

Journal of Ocular Pharmacology and Therapeutics

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145

106

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Research advancements in pharmaceutical sciences have led to the development of new strategies in drug delivery to anterior segment. Designing a new delivery system that can efficiently target the diseased anterior ocular tissue, generate high drug levels, and maintain prolonged and effective concentrations with no or minimal side effects is the major focus of current research. Drug delivery by traditional method of administration via topical dosing is impeded by ocular static and dynamic barriers. Various products have been introduced into the market that prolong drug retention in the precorneal pocket and to improve bioavailability. However, there is a need of a delivery system that can provide controlled release to treat chronic ocular diseases with a reduced dosing frequency without causing any visual disturbances. This review provides an overview of anterior ocular barriers along with strategies to overcome these ocular barriers and deliver therapeutic agents to the affected anterior ocular tissue with a special emphasis on nanotechnology-based drug delivery approaches.

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Section: Cyclodextrinsmentioning

confidence: 99%

Section: Formulation Approaches For Anterior Chamber Deliverymentioning

confidence: 99%

Section: Formulation Approaches For Anterior Chamber Deliverymentioning

confidence: 99%

See 1 more Smart Citation

Novel Strategies for Anterior Segment Ocular Drug Delivery

Cholkar

Patel

Vadlapudi

et al. 2013

Journal of Ocular Pharmacology and Therapeutics

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145

106

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“…Ocular drug delivery is impeded from delivering therapeutic concentrations of drug due to ocular static and dynamic barrier which includes tear/tear dilution (33). CMC is a critical factor that regulates premature release of drug due to tear dilution after topical drop administration.…”

Section: Critical Micellar Concentrationmentioning

confidence: 99%

Optimization of Dexamethasone Mixed Nanomicellar Formulation

et al. 2014

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Abstract. The purpose of this study was to develop a clear aqueous mixed nanomicellar formulation (MNF) of dexamethasone utilizing both D-α-tocopherol polyethylene glycol-1000 succinate (Vit E TPGS) and . In this study, Vit E TPGS and Oc-40 are independent variables. Formulations were prepared following solvent evaporation method. A three level full-factorial design was applied to optimize the formulation based on entrapment efficiency, size, and polydispersity index (PDI). A specific blend of Vit E TPGS and Oc-40 at a particular wt% ratio (4.5:2.0) produced excellent drug entrapment, loading, small mixed nanomicellar size and narrow PDI. Solubility of DEX in MNF is improved by~6.3-fold relative to normal aqueous solubility. Critical micellar concentration (CMC) for blend of polymers (4.5:2.0) was found to be lower (0.012 wt%) than the individual polymers (Vit E TPGS (0.025 wt%) and Oc-40 (0.107 wt%)). No significant effect on mixed nanomicellar size and PDI with one-factor or multifactor interactions was observed. Qualitative 1 H NMR studies confirmed absence of free drug in the outer aqueous MNF medium. MNF appeared to be highly stable. Cytotoxicity studies on rabbit primary corneal epithelial cells did not indicate any toxicity suggesting MNF of dexamethasone is safe and suitable for human topical ocular drops after further in vivo evaluations.

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“…6 Topically applied drug/formulation may not only reach anterior tissues but also reach back-of-the-eye tissues. 7 Effective topical drug delivery poses a major challenge due to the presence of various elimination mechanisms and physiological barriers that result in low ocular bioavailability. [8][9][10] Increasing the retention time in the precorneal area and improving the permeability across ocular tissues of drugs are two major key aspects to enhance ocular bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Functional intercalated nanocomposites with chitosan-glutathione-glycylsarcosine and layered double hydroxides for topical ocular drug delivery

Xu¹,

Xu²,

Gu³

et al. 2018

IJN

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Background To enhance ocular bioavailability, the traditional strategies have focused on prolonging precorneal retention and improving corneal permeability by nano-carriers with positive charge, thiolated polymer, absorption enhancer and so on. Glycylsarcosine (GS) as an active target ligand of the peptide tranpsporter-1 (PepT-1), could specific interact with the PepT-1 on the cornea and guide the nanoparticles to the treating site. Purpose The objective of the study was to explore the active targeting intercalated nanocomposites based on chitosan-glutathione-glycylsarcosine (CG-GS) and layered double hydroxides (LDH) as novel carriers for the treatment of mid-posterior diseases. Materials and methods CG-GS-LDH intercalated nanocomposites were prepared by the coprecipitation hydrothermal method. In vivo precorneal retention study, ex vivo fluorescence images, in vivo experiment for distribution and irritation were studied in rabbits. The cytotoxicity and cellular uptake were studied in human corneal epithelial primary cells (HCEpiC). Results CG-GS-LDH nanocomposites were prepared successfully and characterized by FTIR and XRD. Experiments with rabbits showed longer precorneal retention and higher distribution of fluorescence probe/model drug. In vitro cytological study, CG-GS-LDH nanocomposites exhibited enhanced cellular uptake compared to pure drug solution. Furthermore, the investigation of cellular uptake mechanisms demonstrated that both the active transport by PepT-1 and clathrin-mediated endocytosis were involved in the internalization of CG-GS-LDH intercalated nanocomposites. An ocular irritation study and a cytotoxicity test indicated that these nanocomposites produced no significant irritant effects. Conclusions The active targeting intercalated nanocomposites could have great potential for topical ocular drug delivery due to the capacity for prolonging the retention on the ocular surface, enhancing the drug permeability through the cornea, and efficiently delivering the drug to the targeted site.

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Novel Nanomicellar Formulation Approaches for Anterior and Posterior Segment Ocular Drug Delivery

Cited by 152 publications

References 89 publications

Novel Strategies for Anterior Segment Ocular Drug Delivery

Novel Strategies for Anterior Segment Ocular Drug Delivery

Optimization of Dexamethasone Mixed Nanomicellar Formulation

Functional intercalated nanocomposites with chitosan-glutathione-glycylsarcosine and layered double hydroxides for topical ocular drug delivery

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