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A curcumin-loaded liquid crystal precursor mucoadhesive system for the treatment of vaginal candidiasis.

Salmazi R, Calixto G, Bernegossi J, Ramos MA, Bauab TM, Chorilli M - Int J Nanomedicine (2015)

Bottom Line: Polarized light microscopy and rheological studies revealed that F behaved like an isotropic formulation, whereas F30 and F100 behaved like an anisotropic liquid crystalline system (LCS).Moreover, F30 and F100 presented higher mucoadhesion to porcine vaginal mucosa than F.The analysis of the in vitro activity against Candida albicans revealed that CUR-loaded F was more potent against standard and clinical strains compared with a CUR solution.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, UNESP - Sao Paulo State University, Campus Araraquara, Department of Drugs and Medicines, Araraquara, Sao Paulo, Brazil.

ABSTRACT
Women often develop vaginal infections that are caused primarily by organisms of the genus Candida. The current treatments of vaginal candidiasis usually involve azole-based antifungals, though fungal resistance to these compounds has become prevalent. Therefore, much attention has been given to molecules with antifungal properties from natural sources, such as curcumin (CUR). However, CUR has poor solubility in aqueous solvents and poor oral bioavailability. This study attempted to overcome this problem by developing, characterizing, and evaluating the in vitro antifungal action of a CUR-loaded liquid crystal precursor mucoadhesive system (LCPM) for vaginal administration. A low-viscosity LCPM (F) consisting of 40% wt/wt polyoxpropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, 50% wt/wt oleic acid, and 10% wt/wt chitosan dispersion at 0.5% with the addition of 16% poloxamer 407 was developed to take advantage of the lyotropic phase behavior of this formulation. Notably, F could transform into liquid crystal systems when diluted with artificial vaginal mucus at ratios of 1:3 and 1:1 (wt/wt), resulting in the formation of F30 and F100, respectively. Polarized light microscopy and rheological studies revealed that F behaved like an isotropic formulation, whereas F30 and F100 behaved like an anisotropic liquid crystalline system (LCS). Moreover, F30 and F100 presented higher mucoadhesion to porcine vaginal mucosa than F. The analysis of the in vitro activity against Candida albicans revealed that CUR-loaded F was more potent against standard and clinical strains compared with a CUR solution. Therefore, the vaginal administration of CUR-loaded LCPMs represents a promising platform for the treatment of vaginal candidiasis.

No MeSH data available.


Related in: MedlinePlus

Frequency sweep profiles of unloaded and CUR-loaded formulations.Notes: (A) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (opened symbols) of the unloaded formulations F (▲), F30 (•), and F100 (■). (B) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (open symbols) of the CUR-loaded formulations FC (▲), FC30 (•), and FC100 (■). The SDs have been omitted for clarity; however, in all cases, the coefficients of variation of the triplicate analyses were less than 10%. The data were collected at 37°C±0.5°C.Abbreviations: CUR, curcumin; SD, standard deviation.
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f5-ijn-10-4815: Frequency sweep profiles of unloaded and CUR-loaded formulations.Notes: (A) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (opened symbols) of the unloaded formulations F (▲), F30 (•), and F100 (■). (B) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (open symbols) of the CUR-loaded formulations FC (▲), FC30 (•), and FC100 (■). The SDs have been omitted for clarity; however, in all cases, the coefficients of variation of the triplicate analyses were less than 10%. The data were collected at 37°C±0.5°C.Abbreviations: CUR, curcumin; SD, standard deviation.

Mentions: The oscillatory analyses of all formulations are shown in Figure 5, in which the storage modulus G′ and the loss modulus G″ are plotted against the frequency.


A curcumin-loaded liquid crystal precursor mucoadhesive system for the treatment of vaginal candidiasis.

Salmazi R, Calixto G, Bernegossi J, Ramos MA, Bauab TM, Chorilli M - Int J Nanomedicine (2015)

Frequency sweep profiles of unloaded and CUR-loaded formulations.Notes: (A) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (opened symbols) of the unloaded formulations F (▲), F30 (•), and F100 (■). (B) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (open symbols) of the CUR-loaded formulations FC (▲), FC30 (•), and FC100 (■). The SDs have been omitted for clarity; however, in all cases, the coefficients of variation of the triplicate analyses were less than 10%. The data were collected at 37°C±0.5°C.Abbreviations: CUR, curcumin; SD, standard deviation.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4525803&req=5

f5-ijn-10-4815: Frequency sweep profiles of unloaded and CUR-loaded formulations.Notes: (A) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (opened symbols) of the unloaded formulations F (▲), F30 (•), and F100 (■). (B) Frequency sweep profile of the storage modulus G′ (closed symbols) and loss modulus G″ (open symbols) of the CUR-loaded formulations FC (▲), FC30 (•), and FC100 (■). The SDs have been omitted for clarity; however, in all cases, the coefficients of variation of the triplicate analyses were less than 10%. The data were collected at 37°C±0.5°C.Abbreviations: CUR, curcumin; SD, standard deviation.
Mentions: The oscillatory analyses of all formulations are shown in Figure 5, in which the storage modulus G′ and the loss modulus G″ are plotted against the frequency.

Bottom Line: Polarized light microscopy and rheological studies revealed that F behaved like an isotropic formulation, whereas F30 and F100 behaved like an anisotropic liquid crystalline system (LCS).Moreover, F30 and F100 presented higher mucoadhesion to porcine vaginal mucosa than F.The analysis of the in vitro activity against Candida albicans revealed that CUR-loaded F was more potent against standard and clinical strains compared with a CUR solution.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, UNESP - Sao Paulo State University, Campus Araraquara, Department of Drugs and Medicines, Araraquara, Sao Paulo, Brazil.

ABSTRACT
Women often develop vaginal infections that are caused primarily by organisms of the genus Candida. The current treatments of vaginal candidiasis usually involve azole-based antifungals, though fungal resistance to these compounds has become prevalent. Therefore, much attention has been given to molecules with antifungal properties from natural sources, such as curcumin (CUR). However, CUR has poor solubility in aqueous solvents and poor oral bioavailability. This study attempted to overcome this problem by developing, characterizing, and evaluating the in vitro antifungal action of a CUR-loaded liquid crystal precursor mucoadhesive system (LCPM) for vaginal administration. A low-viscosity LCPM (F) consisting of 40% wt/wt polyoxpropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, 50% wt/wt oleic acid, and 10% wt/wt chitosan dispersion at 0.5% with the addition of 16% poloxamer 407 was developed to take advantage of the lyotropic phase behavior of this formulation. Notably, F could transform into liquid crystal systems when diluted with artificial vaginal mucus at ratios of 1:3 and 1:1 (wt/wt), resulting in the formation of F30 and F100, respectively. Polarized light microscopy and rheological studies revealed that F behaved like an isotropic formulation, whereas F30 and F100 behaved like an anisotropic liquid crystalline system (LCS). Moreover, F30 and F100 presented higher mucoadhesion to porcine vaginal mucosa than F. The analysis of the in vitro activity against Candida albicans revealed that CUR-loaded F was more potent against standard and clinical strains compared with a CUR solution. Therefore, the vaginal administration of CUR-loaded LCPMs represents a promising platform for the treatment of vaginal candidiasis.

No MeSH data available.


Related in: MedlinePlus