Griseofulvin solvate solid dispersions with synergistic effect against fungal biofilms

Abstract

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Development of a Solid Dispersion of Nystatin with Maltodextrin as a Carrier Agent: Improvements in Antifungal Efficacy against Candida spp. Biofilm Infections

“…Recent assays have revealed an enhancement in the antifungal activity of griseofulvin when formulated as a solid dispersion [ 13 ]. Our initial hypothesis, that the hyperosmotic effect of MD would increase the antifungal effect of NYS, has been confirmed.…”

“…This technique is based on the dispersion of poorly water-soluble drugs into a hydrophilic carrier, creating a dispersed state with improved solubility [ 12 ]. Solvent evaporation methods [ 13 , 14 ], spray drying methods [ 9 ], fusion [ 15 ], and fusion/extrusion [ 16 ] have been commonly employed for the production of solid dispersions. In many cases, the solubility increase for these systems was related to the crystallinity decrease by the inclusion of drug molecules within the carrier chains [ 14 , 17 ].…”

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

“…The low solubility of griseofulvin, which is one of the antimicrobials generally used in the treatment of dermatophytosis caused by the fungus Trichophyton rubrum , makes oral administration of its formulation particularly difficult, requiring high doses to reach therapeutic levels. To get around this problem, Al-Obaidi et al [ 37 ] have successfully increased the solubility of this drug developing forms of solvates, also known as pseudopolymorphs, consisting of drug crystals with solvents, stabilized within polymeric matrices. To obtain solid dispersions, different solvated (chloroform) and unsolvated (methanol and acetone) materials were used, including microcrystalline cellulose, PVP K30 and hydroxypropyl methylcellulose acetate succinate (HPMCAS).…”

Solubility Improvement of Progesterone from Solid Dispersions Prepared by Solvent Evaporation and Co-milling

“…From the chemical structures shown in Figure 1, the ability for H-bonding between drug and polymers can be deduced. HPMC and HPMCAS form H-bonds by offering protons and have been found to produce solid dispersions with improved drug solubility [19]. MCC has H-bond donors and has been found to increase ibuprofen solubility and dissolution by co-milling with the drug [27].…”

“…Five excipients were compared: hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP) and silica (SiO 2 ). They were selected on the basis of their different molecular characteristics: HPMC, HPMCAS and PVP are amorphous but PVP does not have H-bond donor groups, whereas the other two polymers have, MCC is semicrystalline with H-bond donors, and silica is amorphous with an ability to accept protons and form H-bonds [19]. In addition, these polymers are commonly used excipients for oral drug delivery, and enhancement of aqueous solubility based on these polymers will be of great interest to pharmaceutical formulation scientists.…”