Design and evaluation of pharmaceutical availability, stability and quality of modified viscosity eye drops with choline salicylate

Wróblewska, K.; Plewa, Szymon; Długaszewska, Jolanta; Froelich, Anna; Muszalska-Kolos, Izabela

doi:10.1016/j.ejps.2021.105725

Cited by 4 publications

(16 citation statements)

References 10 publications

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“…The penetration rate of CS from the eye drops and the CS solution in isotonic sodium chloride solution was assessed using a hydrophilic membrane made of regenerated cellulose (Visking ® ) and a porcine cornea. The CS content in the acceptor part of the Franz cell (volume 8 mL, penetration area 1 cm 2 ) was determined by the UV method [ 26 ]. The blank test confirmed that the solutions of the acceptor part did not show UV absorption in the region of interest (blank sample absorbance was ˂0.004).…”

Section: Resultsmentioning

confidence: 99%

“…Acetylsalicylic acid is a powerful drug with known anti-inflammatory activity [ 22 ] that is also used, particularly as a combined therapy, in ocular surface inflammatory disease [ 23 ], glaucoma treatment [ 24 ], and acute central serous chorioretinopathy [ 25 ]. Thus, there is increased interest in the possibility of using choline salicylate, which is more advantageous in terms of physicochemical properties than acetylsalicylic acid, as an active ingredient of ocular anti-inflammatory drops [ 26 ]. As a nonacetylated derivative of salicylic acid, choline salicylate is classified as a first-generation nonsteroidal anti-inflammatory drug.…”

Section: Introductionmentioning

confidence: 99%

“…The studies conducted on the penetration of CS through hydrophilic membranes and the porcine cornea have confirmed the possibility of its penetration into the corneal structures, justifying the research on the development of an ophthalmic drug. Our previous study showed that the combination of CS and HPMC in eye drops met the quality criteria: pH, viscosity, and osmolarity, as well as in terms of microbiological purity [ 26 ]. HA has several advantages, including mucoadhesive, moisturizing, lubricating, antioxidizing, and anti-inflammatory properties [ 9 , 10 ], which are important for ophthalmological drugs.…”

Section: Introductionmentioning

confidence: 99%

“…Earlier studies on the use of CS eye drops [ 27 ], and the results of the stability of CS and HPMC eye drops [ 26 ], justify the need for further research to improve formulation and the technology of eye drops combining choline salicylate with hyaluronic acid. For this purpose, the technology of preparing sterile eye drops containing CS (2%) and HA (0.4%) as a viscosity-enhancing agent was developed.…”

Section: Introductionmentioning

confidence: 99%

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Novel Formulation of Eye Drops Containing Choline Salicylate and Hyaluronic Acid: Stability, Permeability, and Cytotoxicity Studies Using Alternative Ex Vivo and In Vitro Models

et al. 2021

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This work investigated the potential of a novel formulation of eye drops containing a non-steroidal anti-inflammatory drug—choline salicylate (CS)—and hyaluronic acid (HA). Thus, these drops may exert both anti-inflammatory and regenerative activity. The experiment was conducted through the careful characterization of physicochemical properties, stability, and quality of eye drops. Moreover, microbiological analysis, as well as penetration and cytotoxic studies, were performed. The UV, HPLC-UV, and HPLC-MS/MS methods were used to determine the purity and stability of CS. The penetration rate of CS was assessed using a hydrophilic membrane and ex vivo porcine cornea model. Additionally, the cytotoxic effects were evaluated using the SIRC cell line. The interaction between HA and CS was tested using size-exclusion chromatography and IR spectrophotometry. As a result, HA increased the viscosity of the drops, which prolonged their contact with the ocular surface, thus ensuring more effective penetration of CS into the corneal structure. After long-term storage, an interaction in the pharmaceutical phase between CS and HA was observed. However, this interaction did not affect the viability of rabbit corneal cells. Our findings showed that eye drops with CS and HA, stored at 2–8 °C in light-protected conditions, met the criteria of stability and safety.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Novel Formulation of Eye Drops Containing Choline Salicylate and Hyaluronic Acid: Stability, Permeability, and Cytotoxicity Studies Using Alternative Ex Vivo and In Vitro Models

et al. 2021

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“…Citicoline eye drops were applied to the recovery of corneal sensitivity after laser in situ keratomileusis by enhancing corneal innervation [ 57 ]. Choline salicylate has been developed to increase the viscosity of eye drops [ 58 ]. Nitrogen mustard, which is a vesicant responsible for irreversible corneal injury, damages the corneal epithelium and stroma through the sphingomyelin–ceramide pathway [ 59 ].…”

Section: Choline In Dry Eye Syndrome and Ocular Surfacementioning

confidence: 99%

Role of Choline in Ocular Diseases

Hwang

Shin

2021

IJMS

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Choline is essential for maintaining the structure and function of cells in humans. Choline plays an important role in eye health and disease. It is a precursor of acetylcholine, a neurotransmitter of the parasympathetic nervous system, and it is involved in the production and secretion of tears by the lacrimal glands. It also contributes to the stability of the cells and tears on the ocular surface and is involved in retinal development and differentiation. Choline deficiency is associated with retinal hemorrhage, glaucoma, and dry eye syndrome. Choline supplementation may be effective for treating these diseases.

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Balsam Poplar Buds: Extraction of Potential Phenolic Compounds with Polyethylene Glycol Aqueous Solution, Thermal Sterilization of Extracts and Challenges to Their Application in Topical Ocular Formulations

et al. 2022

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Phenolic compounds of natural origin have been valued for their beneficial effects on health since ancient times. During our study, we performed the extraction of phenolic compounds from balsam poplar buds using different concentrations of aqueous polyethylene glycol 400 solvents (10–30% PEG400). The aqueous 30% PEG400 extract showed the best phenolic yield. The stability of the extract during autoclave sterilization was evaluated. The extract remained stable under heat sterilization. Ophthalmic formulations are formed using different concentrations (8–15%) of poloxamer 407 (P407) together with hydroxypropyl methylcellulose (0.3%), sodium carboxymethyl cellulose (0.3%) or hyaluronic acid (0.1%). Physicochemical parameters of the formulations remained significantly unchanged after sterilization. Formulations based on 12% P407 exhibited properties characteristic of in situ gels, the gelation point of the formulations was close to the temperature of the cornea. After evaluating the amount of released compounds, it was found that, as the concentration of polymers increases, the amount of released compounds decreases. Formulations based on 15% P407 released the least biologically active compounds. Sterilized formulations remained stable for 30 days.

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Design and evaluation of pharmaceutical availability, stability and quality of modified viscosity eye drops with choline salicylate

Cited by 4 publications

References 10 publications

Novel Formulation of Eye Drops Containing Choline Salicylate and Hyaluronic Acid: Stability, Permeability, and Cytotoxicity Studies Using Alternative Ex Vivo and In Vitro Models

Novel Formulation of Eye Drops Containing Choline Salicylate and Hyaluronic Acid: Stability, Permeability, and Cytotoxicity Studies Using Alternative Ex Vivo and In Vitro Models

Role of Choline in Ocular Diseases

Balsam Poplar Buds: Extraction of Potential Phenolic Compounds with Polyethylene Glycol Aqueous Solution, Thermal Sterilization of Extracts and Challenges to Their Application in Topical Ocular Formulations

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