Liposomal amphotericin B eye drops to treat fungal keratitis: Physico-chemical and formulation stability

Self-aggregated nanoparticles based on amphiphilic poly(lactic acid)-grafted-chitosan copolymer for ocular delivery of amphotericin B

“…The lids were then gently held together for 10 seconds and released. The blink rate, discomfort (redness and irritation), discharge rate, and swelling of the cornea and conjunctiva were examined for one day at regular intervals of 1,3,6,8,12, and 24 hours.…”

“…1 Amphotericin B is a macrocyclic polyene antibiotic with a broad antifungal spectrum and remains the drug of first choice for fungal infections caused by yeast. 2,3 Currently, there are no licensed topical formulations containing amphotericin B, and extemporaneous preparations of amphotericin B as eye drops (0.1%-0.3%) from available marketed parenteral formulations (Fungizone New York, NY, USA) are used frequently in the clinic. However, this type of amphotericin B formulation usually has poor clinical efficacy in the treatment of fungal keratitis for several reasons.…”

“…8 Moreover, frequent application of amphotericin B eye drops containing deoxycholate is irritating to the cornea, which would decrease patient compliance, causing treatment failure and emergence of drug resistance. 3,9 As a result of these factors, the bioavailability of the drug is extremely low. Only 1%-5% of the applied active ingredient is available to the ocular tissue and the rest would reach the systemic circulation via the conjunctiva and tear flow in the nasal passage, with undesirable side effects.…”

Amphotericin-B entrapped lecithin/chitosan nanoparticles for prolonged ocular application

“…Literature survey revealed that several approaches were reported for the ocular delivery of AmB using collagen shields [14], intracameral injection [15][16][17][18], solubilised AmB using cyclodextrins [13], liposomal eye drops [19], nanoparticles mediated delivery [20,21], oral delivery through lipid based formulations Table 1 Physico-chemical properties of L/C NPs with different molecular weight CS, each value represents mean ± S.D. (n = 3).…”

Fundamental Aspects in the Development of Microemulsion Systems Containing Amphotericin B for Ophthalmic Use

“…The current formulation of AmB (Fungizone ® ) contains sodium deoxycholate (surfactant needed to promote micellization of AmB) causes during instillation, severe pain (irritability) which lead to non -adherence to the treatment by the patient and consequently, worsening of symptoms 9 . This toxicity associated with the topical ocular administration, may develop through blepharitis, keratitis, and iritis that according to the literature, relates to this surfactant and can be significantly reduced when the lipid formulations are used as vehicles for the incorporation of the drug without the use of this substance 10,11 .…”