Poly(Ethylene Glycol)-block-Poly(ε-Caprolactone) Nanomicelles for the Solubilization and Enhancement of Antifungal Activity of Sertaconazole
Ghareb M. Soliman,
Mohamed A. Attia,
Ramadan A. Mohamed.
Sertaconazole nitrate is a broad spectrum imidazole antifungal agent with antibacterial and anti-inflammatory
properties. However, its lipophilic nature and very poor aqueous solubility limit its use in the clinic. The aim of this study
was to develop and characterize poly(ethylene glycol)-block-poly(ε-caprolactone) (PEG-b-PCL) polymeric nanomicelles
for the solubilization and enhancement of sertaconazole antifungal activity. Sertaconazole was incorporated into PEG-b-
PCL polymeric nanomicelles by a co-solvent evaporation method and micelle size, drug loading capacity and drug release
properties were determined. The antifungal properties of nanomicelle-loaded drug were evaluated in Fusarium miscanthi,
Microsporum canis, and Trichophyton mentagrophytes isolated, respectively from fungal keratitis, ringworm, and tinea
corporis. PEG-b-PCL formed nanomicelles in aqueous solution with a diameter ranging from 40-80 nm, depending on the
polymer composition and level of drug loading. Drug loading properties of the nanomicelles were dependent on the PCL
block molecular weight and drug/polymer weight feed ratio. Drug encapsulation efficiency of up to 85% was achieved
and this resulted in more than 80-fold enhancement in sertaconazole aqueous solubility at polymer concentration of 0.2%.
Drug release studies showed an initial burst release followed by sustained drug release for 72 hours. In vitro antimycotic
studies showed that nanomicelle-incorporated sertaconazole inhibited fungal growth in a concentration dependent manner.
Further, it was more effective than the free drug in inhibiting the growth of Fusarium miscanthi and Microsporum canis.
These results confirm the utility of PEG-b-PCL nanomicelles in enhancing the aqueous solubility and antifungal activity
of sertaconazole or other similar antifungal drugs.
Keywords: Antifungal, fungal infections, polycaprolactone, polymeric nanomicelles, sertaconazole, solubilization.
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