Cysteamine indications and liposomal dosage forms

Indications of Cysteamine

Cysteamine is an orphan drug used in the treatment of cystine deposition disorders to prevent the long-term accumulation of cystine in lysosomes. It is an aminothiol drug and is indicated for the treatment of nephropathic cystinosis and cystinuria.Cysteamine 5% cream is a skin lightening agent used to treat hyperpigmentation disorders such as melasma, post-inflammatory hyperpigmentation and freckles. It is also used to lighten overall skin colour.

liposomal dosage forms of Cysteamine

Despite the high aqueous solubility of cysteamine, its unpleasant organoleptic properties, hygroscopicity, instability in solutions, and poor pharmacokinetic profile are the main drawbacks that limit its use for medical and cosmetic purposes. In this study, cysteamine-loaded liposomes were prepared using the ethanol injection method. Liposomes were characterized for their size, homogeneity, surface charge, and morphology. The incorporation ratios of cholesterol and phospholipids, the encapsulation efficiency and the loading ratio of cysteamine in liposomes were determined. Moreover, the stability of free and encapsulated cysteamine was assessed at different temperatures (4, 25, and 37 °C) in the presence and absence of light. Cysteamine-loaded liposomes were freeze-dried and reconstituted liposomes were characterized. Finally, the storage stability of the freeze-dried cysteamine-loaded liposomes was studied. Liposomes were nanometric, oligolamellar, and spherical. The encapsulation efficiency and the loading ratio of cysteamine varied between 12 and 40% in the different formulations. The encapsulation improved the stability of cysteamine in the various storage conditions. The dried form of cysteamine-loaded liposomes conserved the size of the vesicles and retained 33% of cysteamine present in the liposomal suspension before lyophilization. The freeze-dried liposomes formulations were stable after four months of storage at 4 °C.

References:

[1] CARLA ATALLAH; Catherine C; Hélène Greige Gerges. Development of cysteamine loaded liposomes in liquid and dried forms for improvement of cysteamine stability[J]. International Journal of Pharmaceutics, 2020. DOI:10.1016/j.ijpharm.2020.119721.

[2] CHRISTINA VAN STEIN. A comparison of immediate release and delayed release cysteamine in 17 patients with nephropathic cystinosis.[J]. Orphanet Journal of Rare Diseases, 2021. DOI:10.1186/s13023-021-01991-2.

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