Mucoadhesive Chitosan-Coated Cationic Microemulsion of Dexamethasone for Ocular Delivery:<i>In Vitro</i>and<i>In Vivo</i>Evaluation

Kesavan, Karthikeyan; Kant, Shri; Singh, Paras Nath; Pandit, J. K.

doi:10.3109/02713683.2012.745879

Cited by 73 publications

(30 citation statements)

References 35 publications

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“…Subsequently, several studies of microemulsions with different compositions showed, in vitro and in vivo , an increase in drug penetration in the cornea, tear film and aqueous humour . Studies have also shown a decrease in intraocular pressure, improvement of the miotic response to pilocarpine and improvement in the anti‐inflammatory activity of dexamethasone in the treatment of uveitis …”

Section: Delivery Systemsmentioning

confidence: 99%

Section: Delivery Systemsmentioning

confidence: 99%

“…Recently, some modifications have been made in the formulations of microemulsions with the aim of improving the effectiveness of microemulsions for topical ocular drug delivery . For instance, mucoadhesive chitosan‐coated microemulsions (CH‐MEs) have been investigated for ophthalmic delivery of dexamethasone for uveitis treatment . Chitosan has been widely used in ocular drug delivery because of the interaction between the positively charged chitosan and the negatively charged sialic acid residues of cornea mucin; this interaction can increase the residence time at the ocular surface.…”

Section: Delivery Systemsmentioning

confidence: 99%

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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%

Section: Delivery Systemsmentioning

confidence: 99%

Section: Delivery Systemsmentioning

confidence: 99%

See 1 more Smart Citation

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

show abstract

“…It was initially believed and now has become clearer from many reports in the literature that an occurrence of electrostatic attraction between the cationic emulsified droplets and anionic cellular moieties of the ocular tissues exists [26]. As the corneal area is negatively charged, the positively charged droplets might bind to the sites.…”

Section: Charge Effectmentioning

confidence: 99%

Microemulsion: New Insights into the Ocular Drug Delivery

Hegde

Verma

Ghosh³

2013

ISRN Pharmaceutics

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Delivery of drugs into eyes using conventional drug delivery systems, such as solutions, is a considerable challenge to the treatment of ocular diseases. Drug loss from the ocular surface by lachrymal fluid secretion, lachrymal fluid-eye barriers, and blood-ocular barriers are main obstacles. A number of ophthalmic drug delivery carriers have been made to improve the bioavailability and to prolong the residence time of drugs applied topically onto the eye. The potential use of microemulsions as an ocular drug delivery carrier offers several favorable pharmaceutical and biopharmaceutical properties such as their excellent thermodynamic stability, phase transition to liquid-crystal state, very low surface tension, and small droplet size, which may result in improved ocular drug retention, extended duration of action, high ocular absorption, and permeation of loaded drugs. Further, both lipophilic and hydrophilic characteristics are present in microemulsions, so that the loaded drugs can diffuse passively as well get significantly partitioned in the variable lipophilic-hydrophilic corneal barrier. This review will provide an insight into previous studies on microemulsions for ocular delivery of drugs using various nonionic surfactants, cosurfactants, and associated irritation potential on the ocular surface. The reported in vivo experiments have shown a delayed effect of drug incorporated in microemulsion and an increase in the corneal permeation of the drug.

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“…After three months, CH-ME was subjected to test for physical stability (phase separation) and accelerated centrifugation cycle (5000, 10 000 and 15 000 rpm for 30 min) to observe any change in homogeneity. % T, globule size, zeta potential, pH, viscosity and drug content were monitored over the period of one month, two months and three months (Kesavan et al, 2013).…”

Section: Characterizationmentioning

confidence: 99%

Nose to brain microemulsion-based drug delivery system of rivastigmine: formulation and ex-vivo characterization

et al. 2014

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Alzheimer's disease (AD) is a progressive neurodegenerative disorder leading to irreversible loss of neurons, cognition and formation of abnormal protein aggregates. Rivastigmine, a reversible cholinesterase inhibitor used for the treatment of AD, undergoes extensive first-pass metabolism, thus limiting its absolute bioavailability to only 36% after 3-mg dose. Due to extreme aqueous solubility, rivastigmine shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. This investigation was aimed to formulate microemulsion (ME) and mucoadhesive microemulsions (MMEs) of rivastigmine for nose to brain delivery and to compare percentage drug diffused for both systems using in-vitro and ex-vivo study. Rivastigmine-loaded ME and MMEs were prepared by titration method and characterized for drug content, globule size distribution, zeta potential, pH, viscosity and nasal ciliotoxicity study. Rivastigmine-loaded ME system containing 8% w/w Capmul MCM EP, 44% w/w Labrasol:Transcutol-P (1:1) and 48% w/w distilled water was formulated, whereas 0.3% w/ w chitosan (CH) and cetyl trimethyl ammonium bromide (as mucoadhesive agents) were used to formulate MMEs, respectively. ME and MMEs formulations were transparent with drug content, globule size and zeta potential in the range of 98.59% to 99.43%, 53.8 nm to 55.4 nm and À2.73 mV to 6.52 mV, respectively. MME containing 0.3% w/w CH followed Higuchi model (r 2 ¼ 0.9773) and showed highest diffusion coefficient. It was free from nasal ciliotoxicity and stable for three months. However, the potential of developed CH-based MME for nose to brain delivery of rivastigmine can only be established after in-vivo and biodistribution study.

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Mucoadhesive Chitosan-Coated Cationic Microemulsion of Dexamethasone for Ocular Delivery:In VitroandIn VivoEvaluation

Abstract: The developed CH-MEs are a viable alternative to conventional eye drops for its ability to enhance bioavailability through its longer precorneal residence time and its ability to sustain the release of the drug.

Cited by 73 publications

References 35 publications

Topical delivery of ocular therapeutics: carrier systems and physical methods

Topical delivery of ocular therapeutics: carrier systems and physical methods

Microemulsion: New Insights into the Ocular Drug Delivery

Nose to brain microemulsion-based drug delivery system of rivastigmine: formulation and ex-vivo characterization

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