Tear fluid-eye drops compatibility assessment using surface tension

Grgurević, Martina Hotujac; Juretić, Marina; Hafner, Anita; Lovrić, Jasmina; Pepić, Ivan

doi:10.1080/03639045.2016.1238924

Cited by 32 publications

(27 citation statements)

References 34 publications

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“…This polymer increases the viscosity of the formulation, and as consequence, the retention time of the formulation on the ocular surface [60], but in both cases remained in the range of natural tears. Surface tension values, also in the range of natural precorneal film values (43.6 ± 2.7 mN/m) [40], were low enough to enhance the spreading of the formulation on the ocular surface but not so low as to promote destabilization and damage on the precorneal film [61].…”

Section: Discussionmentioning

confidence: 99%

Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment

Gómez-Ballesteros¹,

López-Cano²,

Bravo‐Osuna

et al. 2019

Polymers

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The combination of acetazolamide-loaded nano-liposomes and Hydroxypropyl methylcellulose (HPMC) with similar components to the preocular tear film in an osmoprotectant media (trehalose and erythritol) is proposed as a novel strategy to increase the ocular bioavailability of poorly soluble drugs. Ophthalmic formulations based on acetazolamide-loaded liposomes, dispersed in the osmoprotectant solution (ACZ-LP) or in combination with HPMC (ACZ-LP-P) were characterized and in vivo evaluated. The pH and tonicity of both formulations resulted in physiological ranges. The inclusion of HPMC produced an increment in viscosity (from 0.9 to 4.7 mPa·s. 64.9 ± 2.6% of acetazolamide initially included in the formulation was retained in vesicles. In both formulations, a similar onset time (1 h) and effective time periods were observed (7 h) after a single instillation (25 μL) in normotensive rabbits’ eyes. The AUC0–8h of the ACZ-LP-P was 1.5-fold higher than of ACZ-LP (p < 0.001) and the maximum hypotensive effect resulted in 1.4-fold higher (p < 0.001). In addition, the formulation of ACZ in the hybrid liposome/HPMC system produced a 30.25-folds total increment in ocular bioavailability, compared with the drug solution. Excellent tolerance in rabbits’ eyes was confirmed during the study.

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Section: Discussionmentioning

confidence: 99%

Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment

Gómez-Ballesteros¹,

López-Cano²,

Bravo‐Osuna

et al. 2019

Polymers

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“…The refractive index values for ACY-AqS and PLGA-TPGS-NPs were close to the refractive index of tear fluid and lachrymal fluid (1.34–1.36) (Craig et al, 1995). The surface tension measurements for ACY-AqS and PLGA-TPGS-NPs were 39.53 ± 1.02 mN·m −1 and 41.28 ± 1.04 mN·m −1 respectively, which are marginally less than the normal range for lachrymal fluid (40–50 mN·m −1 ) (Hotujac Grgurevic et al, 2017, Tiffany et al, 1989) (Table 2-A). Therefore, we assumed that the ACY-AqS and NPs dispersion would mix without any difficulty with precorneal film constituents and would retain satisfactory spreading effect on corneal and precorneal surfaces, which in turn extend the corneal and precorneal retention of the formulations and would improve the ACY ocular bioavailability.…”

Section: Resultsmentioning

confidence: 93%

Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir

Alkholief

Albasit

Alhowyan

et al. 2019

Saudi Pharmaceutical Journal

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Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the poorly soluble Acyclovir topically via ocular route. Our nanosystem is composed of the biocompatible PLGA polymer stabilized with TPGS which possess a high emulsifying capacity and is also known as P-gp inhibitor. The optimized nanoparticles were prepared with 0.3% TPGS and had particle-size of 262.3 nm, zeta-potential of +15.14 mV. The physicochemical-characterization, ex vivo transcorneal permeation, ocular-irritation and Acyclovir ocular-availability, following topical ocular application of PLGA-NPs in rabbit eyes, were performed. The tested parameters and irritation by Draize’s test suggested the suitability and safety of PLGA-NPs for ocular use. An ultrahigh performance liquid chromatographic method was developed, validated, and applied to quantify Acyclovir in aqueous humor which was shown to be significantly higher (p < 0.05) using the developed nanoparticles as compared to Acyclovir-aqueous suspension following their single topical ocular administration. Noticeable 2.78-, 1.71- and 2.2-times increased values of AUC0–24h, t1/2 (h) and MRT0–24h were found, respectively, with the PLGA-TPGS-NPs as compared to ACY-AqS. These results demonstrate the superiority of delivering Acyclovir using a nanosystem compared to conventional methods.

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“…With a trend for eye drops to have increased viscosity, the eye drop still needs to be dispensable from a bottle and produce drops of the desired size and drug concentration. The surface tension and viscosity of a drop also has important implications for the sensation of the drop on the cornea 155…”

Section: Patient‐focused Considerations For Eye Drop Formulationsmentioning

confidence: 99%

“…A shift toward more viscous eye drops, which are more resistant to lacrimal clearance and blinking may increase bioavailability in theory, however in practice they will be more uncomfortable for the patient, increasing blinking and clearance, and creating blurred vision 155. The potential for longer residence times also raises questions around the use of other ocular devices, such as contact lenses.…”

Section: Patient‐focused Considerations For Eye Drop Formulationsmentioning

confidence: 99%

Material, Immunological, and Practical Perspectives on Eye Drop Formulation

Bennett

Chinnery

Downie

et al. 2020

Adv Funct Materials

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Eye drops are the most common and inexpensive approach to topical ocular drug delivery. Eye drops offer a noninvasive treatment strategy; however, this can be detrimental to therapeutic efficacy when compared to invasive methods such as surgeries, implants, and injections. Improvements to the efficacy of the topical delivery of drugs to ocular tissues are currently being explored and much of this work centers on adjusting the formulation of the eye drops and prolonging the bioavailability of the therapeutic agent. This is often in preference to improving other patient‐focused or clinical factors. In this progress report, conventional, commercially available polymer eye drops are explored and the ability for current and future innovations to maintain the existing benefits of eye drops to the patient is assessed. The final materials and form of the drops (liquid, gel, or other) and the immunological implications for the user are explored. There is currently no consensus for how to most effectively improve the ocular retention and drug delivery capabilities of eye drops, but key issues are highlighted in the context of current methods under development, and potential questions and considerations for future innovations are raised.

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Tear fluid-eye drops compatibility assessment using surface tension

Abstract: Our results provide a rationale for clinical studies aiming to assess the correlation between the eye drops surface tension and the tear film (in)stability.

Cited by 32 publications

References 34 publications

Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment

Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment

Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir

Material, Immunological, and Practical Perspectives on Eye Drop Formulation

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