Ex-vivo permeation study of indomethacin from a submicron emulsion through albino rabbit cornea

Muchtar, S.; Abdulrazik, Muhammad; Frucht‐Pery, Joseph; Benita, Simon

doi:10.1016/s0168-3659(96)01503-9

Cited by 51 publications

(22 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…128 Indomethacin nanoemulsion prepared with amphoteric surfactant (lauroamphodiacetate) also improved corneal permeability by 3.8 times relative to a marketed product (Indocollyre Ò ). 129 In a recently published patent, CS-A was successfully incorporated in a nanoemulsion, utilizing positively charged polar lipid, such as stearylamine. 130 Mean droplet size of the formulation was within the range of 150-250 nm, with zeta potential of 34-45 mV.…”

Section: Cholkar Et Almentioning

confidence: 99%

Novel Strategies for Anterior Segment Ocular Drug Delivery

Cholkar

Patel

Vadlapudi

et al. 2013

Journal of Ocular Pharmacology and Therapeutics

152

107

View full text Add to dashboard Cite

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.

show abstract

Section: Cholkar Et Almentioning

confidence: 99%

Novel Strategies for Anterior Segment Ocular Drug Delivery

Cholkar

Patel

Vadlapudi

et al. 2013

Journal of Ocular Pharmacology and Therapeutics

152

107

View full text Add to dashboard Cite

show abstract

“…This might be due to the inclusion of triacetin as a cosurfactant in this nanoemulsion. Triacetin, being an oil, increased the oil content of the nanoemulsion which acts as a drug reservoir and so, more oil was available to adhere to the lipophilic surface of the corneal epithelium and so, this could promote dorzolamide hydrochloride penetration (72).…”

Section: Therapeutic Efficacy Studiesmentioning

confidence: 99%

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

et al. 2009

View full text Add to dashboard Cite

Abstract. Dilutable nanoemulsions are potent drug delivery vehicles for ophthalmic use due to their numerous advantages as sustained effect and high ability of drug penetration into the deeper layers of the ocular structure and the aqueous humor. The aim of this article was to formulate the antiglaucoma drug dorzolamide hydrochloride as ocular nanoemulsion of high therapeutic efficacy and prolonged effect. Thirty-six systems consisting of different oils, surfactants, and cosurfactants were prepared and their pseudoternary-phase diagrams were constructed by water titration method. Seventeen dorzolamide hydrochloride nanoemulsions were prepared and evaluated for their physicochemical and drug release properties. These nanoemulsions showed acceptable physicochemical properties and exhibited slow drug release. Draize rabbit eye irritation test and histological examination were carried out for those preparations exhibiting superior properties and revealed that they were nonirritant. Biological evaluation of dorzolamide hydrochloride nanoemulsions on normotensive albino rabbits indicated that these products had higher therapeutic efficacy, faster onset of action, and prolonged effect relative to either drug solution or the market product. Formulation of dorzolamide hydrochloride in a nanoemulsion form offers, thus, a more intensive treatment of glaucoma, a decrease in the number of applications per day, and a better patient compliance compared to conventional eye drops.

show abstract

“…Prolonged residence of oily suspension in the conjunctival sac and favorable partition characteristics of the drug could account for the higher aqueous humor penetration of indomethacin from oily suspension compared with the aqueous suspension. Indomethacin, incorporated into o/w emulsion of medium chain triglyceride(oil phase) stabilized by combination of phospholipids and an amphoteric surfactant, with pH of aqueous phase adjusted to 3.8 was evaluated for corneal permeation through excised rabbit cornea (24). The apparent corneal permeability of indomethacin from the emulsion was found to be 3.8 fold higher than the conventional marketed aqueous formulation.…”

Section: Indole Acetic Acid Derivatives Indomethacinmentioning

confidence: 99%

Topical Ocular Delivery of NSAIDs

Ahuja

Dhake²,

Sharma

et al. 2008

AAPS J

189

148

View full text Add to dashboard Cite

Abstract. In ocular tissue, arachidonic acid is metabolized by cyclooxygenase to prostaglandins which are the most important lipid derived mediators of inflammation. Presently nonsteroidal anti-inflammatory drugs (NSAIDs) which are cyclooxygenase (COX) inhibitors are being used for the treatment of inflammatory disorders. NSAIDs used in ophthalmology, topically, are salicylic-, indole acetic-, aryl acetic-, aryl propionicand enolic acid derivatives. NSAIDs are weak acids with pKa mostly between 3.5 and 4.5, and are poorly soluble in water. Aqueous ophthalmic solutions of NSAIDs have been made using sodium, potassium, tromethamine and lysine salts or complexing with cyclodextrins/solubilizer. Ocular penetration of NSAID demands an acidic ophthalmic solution where cyclodextrin could prevent precipitation of drug and minimize its ocular irritation potential. The incompatibility of NSAID with benzalkonium chloride is avoided by using polysorbate 80, cyclodextrins or tromethamine. Lysine salts and α-tocopheryl polyethylene glycol succinate disrupt corneal integrity, and their use requires caution. Thus a nonirritating ophthalmic solution of NSAID could be formulated by dissolving an appropriate water-soluble salt, in the presence of cyclodextrin or tromethamine (if needed) in mildly acidified purified water (if stability permits) with or without benzalkonium chloride and polyvinyl alcohol. Amide prodrugs met with mixed success due to incomplete intraocular hydrolysis. Suspension and ocular inserts appear irritating to the inflamed eye. Oil drop may be a suitable option for insoluble drugs and ointment may be used for sustained effect. Recent studies showed that the use of colloidal nanoparticle formulations and the potent COX 2 inhibitor bromfenac may enhance NSAID efficacy in eye preparations.

show abstract

Ex-vivo permeation study of indomethacin from a submicron emulsion through albino rabbit cornea

Cited by 51 publications

References 18 publications

Novel Strategies for Anterior Segment Ocular Drug Delivery

Novel Strategies for Anterior Segment Ocular Drug Delivery

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

Topical Ocular Delivery of NSAIDs

Contact Info

Product

Resources

About