Technology of stable, prolonged-release eye-drops containing Cyclosporine A, distributed between lipid matrix and surface of the solid lipid microspheres (SLM)

Wolska, Eliza; Sznitowska, Małgorzata

doi:10.1016/j.ijpharm.2012.11.009

Cited by 20 publications

(30 citation statements)

References 31 publications

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“…In the multicompartment systems like SLM dispersions, one can distinguish four domains where the drug may be localized: the matrix of the lipid particle, the surface of the lipid particle (interphase), micelles and water. The API distribution between these phases is a main feature characterizing the formulation [ 3 , 8 , 9 , 10 ]. The most common approach is to incorporate the API in the lipid matrix; however, the other locations should also be considered, especially when the effectiveness of drug loading is evaluated.…”

Section: Introductionmentioning

confidence: 99%

“…In the case of some SLM or SLN formulations, a significant fraction of the API was found on the surface of the lipid particles [ 4 , 9 ]. This fraction was responsible for the fast drug release phase and the phase of prolonged release related to the fraction of the API incorporated in the lipid matrix [ 5 , 8 , 11 ]. Unfortunately, even drug substances well-soluble in lipids are often excluded from the lipid matrix during the preparation or storage [ 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

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Analytical Techniques for the Assessment of Drug-Lipid Interactions and the Active Substance Distribution in Liquid Dispersions of Solid Lipid Microparticles (SLM) Produced de novo and Reconstituted from Spray-Dried Powders

et al. 2020

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Solid lipid microparticles (SLM) can be presented as liquid suspension or spray-dried powder. The main challenge in SLM technology is to precisely determine the location of the active substance (API) in the different compartments of the formulation and its changes during SLM processing. Therefore, the purpose of the research was to assess the distribution of the API and to investigate the nature of the API-lipid interaction when the formulation was subjected to spray drying, with an indication of the most suitable techniques for this purpose. SLM were prepared with two various lipids (Compritol or stearic acid) and two model APIs: cyclosporine (0.1% and 1% w/w) and spironolactone (0.1% and 0.5% w/w). Physicochemical characterizations of the formulations, before and after spray drying, were performed by differential scanning calorimetry (DSC), atomic force microscopy (AFM), Raman spectroscopy and nuclear magnetic resonance (NMR). The API distribution between the SLM matrix, SLM surface and the aqueous phase was determined, and the release study was performed. It was demonstrated that, in general, the spray drying did not affect the drug release and drug distribution; however, some changes were observed in the SLM with Compritol and when the API concentration was lower. Only in the SLM with stearic acid was a change in the DSC curves noted. Measurements with the AFM technique proved to be a useful method for detecting differences in the surface properties between the placebo and API-loaded SLM, while the Raman spectroscopy did not show such evident differences.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Analytical Techniques for the Assessment of Drug-Lipid Interactions and the Active Substance Distribution in Liquid Dispersions of Solid Lipid Microparticles (SLM) Produced de novo and Reconstituted from Spray-Dried Powders

et al. 2020

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“…[86] Similar results have been obtained using cyclosporine-loaded lipid microspheres, capable of a prolonged release of the medication with cyclosporine concentration much higher than in the traditional ocular emulsion. [268] These results suggest that patients affected by uveitis could potentially benefit from the use of sustained-release drug formulations, representing a way to localized and deliver the drug more efficiently than topical or systemic administration.…”

Section: Ocular Diseasesmentioning

confidence: 99%

Modern Therapeutic Approaches for Noninfectious Ocular Diseases Involving Inflammation

Ratay

Bellotti

Gottardi³

et al. 2017

Adv Healthcare Materials

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Dry eye disease (DED), age-related macular degeneration (AMD), and Uveitis are ocular diseases that significantly affect the quality of life of millions of people each year. In these diseases, the action of chemokines, pro-inflammatory cytokines, and immune cells drives a local inflammatory response that results in ocular tissue damage. Multiple therapeutic strategies have been developed to either address the symptoms or abate the underlying cause of these diseases. Herein, we will review the challenges to deliver drugs to the relevant location in the eye for each of these diseases as well as current and innovative therapeutic approaches that attempt to restore homeostasis within the ocular microenvironment.

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“…CsA was administered for seven consecutive days into rabbit eyes in different formulations (oily solution and lipid dispersed systems) with the drug concentration in the range 0.5-2.0% (Wolska and Sznitowska, 2013). As a control, 0.9% NaCl was also administered.…”

Section: Sample Collectionmentioning

confidence: 99%

“…CsA is successfully applied in ophthalmology, where topical ocular administration of CsA is used in the treatment of the variety of immune‐mediated ocular surface disorders, for the prevention of corneal allograft rejection, and in therapy for dry eye (Hingorani et al ., ; Perry et al ., ; Tang‐Liu and Acheampong, ; Guzey et al ., ). New delivery systems, including nanocarriers, are under development (Diebold and Calonge, ; Wolska and Sznitowska, ) that require the determination of the distribution of the drug within the structures of the eye. The aim of the present study was to develop and validate a new, fast and simple UHPLC method for the quantitative analysis of CsA in ocular tissues.…”

Section: Introductionmentioning

confidence: 99%

Development and validation of UHPLC method for the determination of cyclosporine A in biological samples

Szerkus

Wolska

Struck-Lewicka

et al. 2014

Biomedical Chromatography

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The aim of the study was to develop and validate a simple and rapid method for the determination of cyclosporine A (CsA) in ocular rabbit tissues using reversed-phase ultra-high-performance liquid chromatography (UHPLC) with UV detection. Previous publications on chromatographic methods of CsA determination in ocular tissues involved only reversed-phase HPLC separation, usually in combination with such detection techniques as radio-immunoassay and mass spectrometry. The application of the UHPLC technique allowed us to significantly decrease the analysis time. Cyclosporine D (CsD) was applied as the internal standard. Satisfactory separation was achieved on an XB-C18 Kinetex column at 60°C with the use of gradient elution mode. The retention times of CsA and CsD were found to be 4.5 and 5.1 min, respectively. The developed assay is specific, sensitive (limit of detection = 6 ng/mL and limit of quantitation = 18 ng/mL) and linear within the analyte concentration range of 0.018-5 µg/mL, with a correlation coefficient of 0.999. High sensitivity, low injection volume (10 μL), short time of analysis (6.5 min) and simplicity make this method useful for the fast analysis of CsA in rabbit ocular tissues and fluids: lacrimal fluid, aqueous humor, cornea, conjunctiva and eye globe.

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Technology of stable, prolonged-release eye-drops containing Cyclosporine A, distributed between lipid matrix and surface of the solid lipid microspheres (SLM)

Cited by 20 publications

References 31 publications

Analytical Techniques for the Assessment of Drug-Lipid Interactions and the Active Substance Distribution in Liquid Dispersions of Solid Lipid Microparticles (SLM) Produced de novo and Reconstituted from Spray-Dried Powders

Analytical Techniques for the Assessment of Drug-Lipid Interactions and the Active Substance Distribution in Liquid Dispersions of Solid Lipid Microparticles (SLM) Produced de novo and Reconstituted from Spray-Dried Powders

Modern Therapeutic Approaches for Noninfectious Ocular Diseases Involving Inflammation

Development and validation of UHPLC method for the determination of cyclosporine A in biological samples

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