Ophthalmic Microemulsion: Formulation Design and Process Optimization

Bodkhe, Atul Arvind; Bedi, Ramandeep Singh; Upadhayay, Ashutosh; Kale, Mohan K.

doi:10.5958/0974-360x.2018.00998.8

Cited by 4 publications

(1 citation statement)

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“…The term "Microemulsion" (ME) is defined as the dispersion of water and oil in the presence of a surfactant and cosurfactant mixture (Smix) in a way that lowers interfacial tension and produces small particle sizes (5-200nm) with reduced surface tension. Microemulsion can enhance drug absorption via higher penetration and enhanced solubility (7)(8)(9). Prednisolone acetate (PA) is a synthetic version of the natural corticosteroid hormone produced by the adrenal gland, used to treat a wide range of conditions.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Prednisolone Acetate Microemulsion for Ophthalmic Use

Al-Rubaye,

Al-Kinani

2023

J Fac Med Baghdad

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Background: Prednisolone acetate is an ester form of prednisolone. It is used topically as an ophthalmic suspension to treat many inflammatory ocular conditions, where its absorption from suspension is highly variable and has poor dose accuracy. Objectives: The main objective of this research is to formulate and evaluate prednisolone acetate microemulsion for ophthalmic use to increase solubility, residence time, and corneal permeability of the drug to enhance patient compliance and treatment efficacy. Methods: Twenty-four prednisolone acetate-loaded microemulsion (0.5%w/w) formulas were prepared using oleic acid, isopropyl myristate as (oil phase) (1:1), tween 80, labrasol, and cremophor EL as (surfactant), ethanol, polyethylene glycol 400, propylene glycol, transcutol P as co-surfactant and Sörensen isotonic phosphate buffer saline pH 7.4 as the aqueous phase at different Smix ratios (1:1), (1:2) and (2:1) by aqueous titration method to construct pseudoternary phase diagram to determine the existence of microemulsion region. All the prepared formulas were subjected to different evaluation tests to determine the optimum formula. Results: observations of the microemulsion showed that it had a clear and transparent yellowish color, formulation F9 composed of oleic acid and isopropyl myristate in a ratio (1:1) as oil, twee80 as a surfactant, and propylene glycol: ethanol (1:1) in a ratio (2:1) as cosurfactant gave the best particle size (10.18nm), polydispersity index (0.2216), zeta potential (-25,91), % of transmittance (99.382%±0. 09), and drug content (100±0.16). Microemulsion formulation provided considerably higher permeability than the marketed eye drop suspension (Optipred®) and improved bioavailability. Conclusions: The microemulsion-containing prednisolone acetate is a promising ocular carrier for the controlled release of prednisolone acetate in treating anterior segment inflammation. Received: Dec. 2022 Accepted March 2023 Published: Oct.2023

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Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Prednisolone Acetate Microemulsion for Ophthalmic Use

Al-Rubaye,

Al-Kinani

2023

J Fac Med Baghdad

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Effect of Oleic acid Incorporation on delivery of Carteolol from commercial Silicone contact lenses

Rayya

haushey

2022

RJPT

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Carteolol HCl (CRT) is a non-selective beta blocker used to treat glaucoma. Currently, it is delivered via eye drop solutions, which suffer from many limitations (e.g. low bioavailability, high dose requirements and noncompliance). Contact lenses are used by scientists to control the release of ocular drugs, and they are considered as a promising therapeutic tool. This research aimed to evaluate the effect of oleic acid (OA) incorporation on CRT loading and its release from commercial silicone contact lens using the soaking method. Two different concentrations of oleic acid solution (35 and 60mg/ml) and one concentration of CRT solution (2 mg/ml) were used. Drug release profile and various lens properties including changes in visible light transmittance, water content, lens diameter and tensile modulus were investigated. The two used concentrations of oleic acid solution (35 and 60mg/ml) led to oleic acid loadings of 14.6% and 24% respectively, which in turn enhanced the total amount of released CRT by a factor of about 10 and 18, and increased the 90% drug release time by a factor of about 12 and 56, respectively for AIR OPTIX® lens. As for the characterization of prepared lenses, all the results were acceptable compared with unmodified lenses except for the change in diameter of lenses loaded with 24% of oleic acid. Our findings revealed the potential of using oleic acid to improve the uptake of CRT and to achieve sustained release kinetics without compromising the critical properties of contact lens.

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Role of Surfactant and Co-surfactant in Microemulsion: A Review

Ande

Sonone

Bakal

et al. 2022

RJPT

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Microemulsions are one in all the most effective candidates as novel drug delivery system due to their long time period stability, improved drug solubilization with simple preparation and administration. Surfactants and cosurfactants play crucial role to get stable, mild and clinically acceptable microemulsions in their optimized concentration, The main aim of the study to produce an efficient screening approach for the surfactant and cosurfactant selection for the excipients of microemulsion formulation development and to check the consequences of surfactant hydrophilic–lipophilic balance (HLB) as well solubilization stability process in microemulsion. The composition and extent of surfactants and cosurfactants were key variables for physicochemical properties of drug-loaded Microemulsions. The important aspects must be considered for a successful microemulsion process is that the stability of the liquid membrane. This study is an attempt to grasp the mechanism of the effect of the surfactant and chain length of co-surfactants within the microemulsion base formulation stability.

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Ophthalmic Microemulsion: Formulation Design and Process Optimization

Cited by 4 publications

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Preparation and Characterization of Prednisolone Acetate Microemulsion for Ophthalmic Use

Preparation and Characterization of Prednisolone Acetate Microemulsion for Ophthalmic Use

Effect of Oleic acid Incorporation on delivery of Carteolol from commercial Silicone contact lenses

Role of Surfactant and Co-surfactant in Microemulsion: A Review

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