Pharmaceutical challenges and perspectives in developing ophthalmic drug formulations

Min, Kyung Up; Maharjan, Pooja; Cho, Kwan Hyung; Maharjan, Anjila; Shin, Meong Cheol; Moon, Cheol

doi:10.1007/s40005-018-0404-6

Cited by 31 publications

(16 citation statements)

References 110 publications

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“…Because of the unique pharmacodynamics and pharmacokinetic properties of the eyes, characterized by anatomical structures of anterior and posterior segments, and tear dilution, ophthalmic delivery system faces challenges in administering drugs [1]. Pharmacodynamics and pharmacokinetic properties of the eyes create therapeutic challenges and result in poor ocular bioavailability [2]. Therefore, there is an urgent need for advances in a nanoengineering drug delivery system for an effective delivery of drugs to target sites along with improved ocular bioavailability.…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, there is an urgent need for advances in a nanoengineering drug delivery system for an effective delivery of drugs to target sites along with improved ocular bioavailability. In this respect, different nanoengineered strategies have been investigated to improve the drug delivery system via the ocular route for the treatment of various ocular diseases [2]. Various biocompatible drug carriers have been incorporated to ensure optimal ocular delivery formulations so as to increase effective drug concentrations in anterior or posterior eye tissues.…”

Section: Introductionmentioning

confidence: 99%

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Potential Albumin-Based Antioxidant Nanoformulations for Ocular Protection against Oxidative Stress

et al. 2019

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Amongst various drug administration methods, ophthalmic drug delivery has been a useful way for the treatment of eye-related diseases. However, therapeutic efficacy of ocular therapy for anterior or posterior eye segments through topical administration is considerably challenged by the number of anatomical and physiological barriers in the eyes affecting ocular bioavailability. In this respect, advanced biocompatible nanoformulations make it possible to improve drug delivery to the target sites and enhance ocular bioavailability of ophthalmic medicines. Various ocular diseases have been reported to be related to oxidative stresses in tissues, and polyphenolic compounds have been known for their antioxidant activities in various tissues, including the eyes. Despite drug efficacy, poor water solubility and intrinsic color of the compounds limit the drug’s inclusion into the development of ocular medicine. In the present study, we investigated the antioxidant protectant efficacy of rosmarinic or ursolic acid in the retinal epithelial cells, as compared to those of curcumin, by forming nanospheres with bovine serum albumin. Our results demonstrate that antioxidant-containing nanoformulations provide a significantly higher drug solubility and decreased ROS (reactive oxygen species) production in the retinal epithelial cells. Finally, we also found that albumin-based nanoformulations could improve bioavailability and increase antioxidant activity of rosmarinic or ursolic acid in the retina to be applied as efficient ocular protectant.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Potential Albumin-Based Antioxidant Nanoformulations for Ocular Protection against Oxidative Stress

et al. 2019

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“…In particular, among the formulations containing lubricants, F3 and F4 exhibited better precipitation-inhibiting effects than F2. It was reported that the stability of protein in thermal conditions increases when polymers or sugars are added [40][41][42][43][44]. This thermal resistance can maintain the quality of the eye drop when the formulation is exposed to unexpected thermal conditions.…”

Section: Long-term and Accelerated Testmentioning

confidence: 99%

Achyranthis radix Extract-Loaded Eye Drop Formulation Development and Novel Evaluation Method for Dry Eye Treatment

et al. 2020

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Recently, Achyranthis radix extract has been studied as a therapeutic agent for dry eye disease that occurs from fine dust. The aim of this study was the development of Achyranthis radix extract-loaded eye drop formulations using lubricants, generally used for artificial tear eye drops. Ecdysterone was used as a marker compound for Achyranthis radix extract and 1% Achyranthis radix extract solution contained 14.37 ± 0.04 μg/mL of ecdysterone. Before formulation studies, a new method was performed to evaluate pigmentation, which might be caused by eye drops of herbal extract. A comparative study of the water retention ability of each formulation and ability to prevent the death of conjunctival epithelial cells in dry conditions was conducted. Moreover, treatment of Achyranthis radix extract (USL) eye drop formulation exhibited a significant inhibitory effect on inflammation in a concentration-dependent manner. The long-term and accelerated stability tests showed that lubricants could contribute to the stability of herbal extracts in solution. In conclusion, hyaluronic acid showed a good effect on the development of eye drop formulation using Achyranthis radix extracts for treating dry eye disease.

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“…The generally accepted and less harmful solution to improve therapeutic treatment and drug bioavailability is to the increase the residence time of drop formulations on the ocular surface, thus increasing drug concentration on the cornea and reducing drug waste [12]. This has been achieved with drug-impregnated contact lenses, patches, colloidal carriers (nanoparticles, different kind of liposomes, etc.,), microneedles, films, gels, or solutions of mucoadhesive polymers, which is the simplest method [3,[13][14][15][16][17][18][19][20][21][22][23]. A variety of materials has been used to prepare these smart delivery systems: natural or synthetic polymeric matrices, which can be modified and tuned for specific applications.…”

Section: Introductionmentioning

confidence: 99%

Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments

et al. 2020

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Chitosan (CS) is a hemi-synthetic cationic linear polysaccharide produced by the deacetylation of chitin. CS is non-toxic, highly biocompatible, and biodegradable, and it has a low immunogenicity. Additionally, CS has inherent antibacterial properties and a mucoadhesive character and can disrupt epithelial tight junctions, thus acting as a permeability enhancer. As such, CS and its derivatives are well-suited for the challenging field of ocular drug delivery. In the present review article, we will discuss the properties of CS that contribute to its successful application in ocular delivery before reviewing the latest advances in the use of CS for the development of novel ophthalmic delivery systems. Colloidal nanocarriers (nanoparticles, micelles, liposomes) will be presented, followed by CS gels and lenses and ocular inserts. Finally, instances of CS coatings, aiming at conferring mucoadhesiveness to other matrixes, will be presented.

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Pharmaceutical challenges and perspectives in developing ophthalmic drug formulations

Cited by 31 publications

References 110 publications

Potential Albumin-Based Antioxidant Nanoformulations for Ocular Protection against Oxidative Stress

Potential Albumin-Based Antioxidant Nanoformulations for Ocular Protection against Oxidative Stress

Achyranthis radix Extract-Loaded Eye Drop Formulation Development and Novel Evaluation Method for Dry Eye Treatment

Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments

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