Production and Characterization of a Clotrimazole Liposphere Gel for Candidiasis Treatment

• Main Authors: Elisabetta Esposito, Maddalena Sguizzato, Christian Bories, Claudio Nastruzzi, Rita Cortesi
• Format: Article
• Language: English
• Published: MDPI AG 2018-02-01
• Series: Polymers
• Subjects: clotrimazole; liposphere; alkyl lactate; xanthan gum; Candida albicans; mucoadhesion
• Online Access: http://www.mdpi.com/2073-4360/10/2/160

This study describes the design and characterization of a liposphere gel containing clotrimazole for the treatment of Candida albicans. Lipospheres were produced by the melt-dispersion technique, using a lipid phase constituted of stearic triglyceride in a mixture with caprylic/capric triglyceride or an alkyl lactate derivative. The latter component was added to improve the action of clotrimazole against candida. The liposphere morphology and dimensional distribution were evaluated by scanning electron microscopy. Clotrimazole release kinetics was investigated by an in vitro dialysis method. An anticandidal activity study was conducted on the lipospheres. To obtain formulations with suitable viscosity for vaginal application, the lipospheres were added to a xanthan gum gel. The rheological properties, spreadability, leakage, and adhesion of the liposphere gel were investigated. Clotrimazole encapsulation was always over 85% w/w. The anticandidal study demonstrated that the encapsulation of clotrimazole in lipospheres increased its activity against Candida albicans, especially in the presence of the alkyl lactate derivative in the liposphere matrix. A dialysis method demonstrated that clotrimazole was slowly released from the liposphere gel and that the alkyl lactate derivative further controlled clotrimazole release. Adhesion and leakage tests indicated a prolonged adhesion of the liposphere gel, suggesting its suitability for vaginal application.