Temperature-dependent in Situ Gel of Clotrimazole: an Experimental Study

Abstract

Background: The in-situ gel-forming polymeric formulations offer sustained and prolonged action in comparison to conventional drug delivery systems. Aim: To formulate and evaluate in situ vaginal gel of clotrimazole. Materials and methods: Poloxamer 407 (20%) was slowly added to freezing water (5°C) with constant stirring. The prepared dispersion was refrigerated for 5 h, the different concentrations of polymers were added for preliminary batches. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) were performed for clotrimazole-excipients compatibility study. The final batch was prepared and evaluated for physicochemical parameters, in vitro clotrimazole release, in vitro antifungal activity, and in vivo vaginal tissue irritation test. Results: The compatibility study showed no chemical interaction between clotrimazole and excipients used. The evaluation parameters showed that clotrimazole release was in the range of 8 to 10 h, gelling temperature was in the range of 27–35°C, gelling time was in the range of 28–34 sec, pH was in the range of 4.4–4.8, and viscosities were in the range of 16.4–182.6 cP (solution form) and 10,500–20,756 cP (gel form). The zone of inhibitions for clotrimazole pure drug, the marketed vaginal gel of clotrimazole, and optimized gel formulation was 9.15±0.75 mm, 14.35±1.12 mm, and 18.85±1.56 mm, respectively (p < 0.0001, q = 5.98). An optimized gel formulation was not irritant to vaginal tissue. Conclusion: It was possible to formulate effective in situ vaginal gel for control release action of clotrimazole. Level of Evidence: IIC.

Fabrication and Characterization of Chitosan/Poly(Lactic-Co-glycolic Acid) Core-Shell Nanoparticles by Coaxial Electrospray Technology for Dual Delivery of Natamycin and Clotrimazole

“…The presence of NAT is confirmed by the characteristic adsorption band and peaks due to the conjugated ester absorption band, primary amine, and cyclic ether (Phan et al, 2014) of the copolymer at 1,716, 1,571, and 1,003 cm −1 , respectively. In addition, the peaks observed at 3,058 and 740 cm −1 are attributed to the C-H aromatic stretch and C-H stretching of CLZ while the peaks at 1,590 and 1,490 cm −1 are related to the CLZ benzene ring stretching (Patel et al, 2019). Meanwhile, the FTIR spectra of electro-sprayed NPs each exhibit outstanding absorption bands in the range of 3,500-3,300 cm −1 , corresponding to the -OH group of CTS along with a peak (at ∼1,760 cm −1 ) associated with the C = O stretching of PLGA ( Figure 3B).…”

In Vitro Performance Analysis of a Minoxidil Thermosensitive Gel with Reduced Runoff for Eyebrow Hair Growth

“…The rheological behavior of the formulation is also critical for droplet dosing, transition temperature, drug-delivered dose, and application comfort, consequently affecting the treatment efficacy and patient compliance [ 25 ].…”

Recent Advances in Nanosystems and Strategies for Vaginal Delivery of Antimicrobials

“…All the tested samples had gelling time in the 2-34 seconds range. In summary, developed systems were simple and easy to use, syringable, allowed easy insertion of gel formulation into the vagina, and were able to release clotrimazole in a controlled way for a prolonged period of time [92].…”