Application of hydrophilic polymers for the preparation of tadalafil solid dispersions: micromeritics properties, release and erectile dysfunction studies in male rats

Abstract

The objective of the present study was to improve the dissolution rate and aphrodisiac activity of tadalafil by using hydrophilic polymers. Solid dispersions were prepared by solvent evaporation-Rota evaporator using Koliphore 188, Kollidon® VA64, and Kollidon® 30 polymers in a 1:1 ratio. Prepared tadalafil-solid dispersions (SDs) evaluated for yield, drug content, micromeritics properties, physicochemical characterizations, and aphrodisiac activity assessment. The optimized SDs TK188 showed size (2.175 ± 0.24 µm), percentage of content (98.89 ± 1.23%), yield (87.27 ± 3.13%), bulk density (0.496 ± 0.005 g/cm3), true density (0.646 ± 0.003 g/cm3), Carr’s index (23.25 ± 0.81), Hausner ratio (1.303 ± 0.003) and angle of repose (<25°). FTIR spectrums revealed tadalafil doesn’t chemically interact with used polymers. XRD and DSC analysis represents TK188 SDs were in the amorphous state. Drug release was 97.17 ± 2.43% for TK188, whereas it was 32.76 ± 2.65% for pure drug at the end of 2 h with 2.96-fold increase in dissolution and followed release kinetics of Korsmeyer Peppa’s model. MDT and DE were noted to be 17.48 minutes and 84.53%, respectively. Furthermore, TK188 SDs showed relative improvement in the sexual behavior of the male rats. Thus the developed SDs TK188 could be potential tadalafil carriers for the treatment of erectile dysfunction.

Enhanced Apigenin Dissolution and Effectiveness Using Glycyrrhizin Spray-Dried Solid Dispersions Filled in 3D-Printed Tablets

“…Similarity index results of the dissolution profiles of a 3D printlet (APN2) before and after undergoing stability testing (Figure 12). The results indicate an f2 value of approximately 70.59, which is a measure of the similarity between the two dissolution profiles [44,45].…”

Development and Characterization of Chitosan-Based Spray-Dried Solid Dispersions of Apigenin: 3D Printed Shell-Pill for Improved Efficacy of Model Flavonoid

“…The resulting powder consists of drug-polymer particles in a solid state called spray dried solid dispersions (SDSDs) [35]. MM Ahmed et al reported the improved dissolution and aphrodisiac activity of sildenafil and tadalafil SDSDs using glycyrrhizin [36], [37], [31]. Spray-dried amorphous solid dispersion of diosmin in soluplus was prepared by MK Anwer and reported to show improved hepato-renoprotective and anti-oxidant properties [38].…”

“…Pharma test automated powder flow analyzer was used (PTG-S4 Hainburg Germany) to measure the angle of repose (𝞱𝞱). The 𝞱𝞱 is an angle between the surface of the pile and the horizontal plane [37]. 𝞱𝞱 = 𝑪𝑪𝑪𝑪𝒊𝒊 −𝟏𝟏 𝒘𝒘 𝑷𝑷 ⁄…”

Development and evaluation of sildenafil/glycyrrhizin-loaded nanofibers as a potential novel buccal delivery system for erectile dysfunction

“…Aldawsari et al have prepared solid dispersions of sildenafil using hydrophilic polymers such as Kollidon® 30, Kolliphor® P188, and Kollidon and demonstrated enhanced dissolution rate, and significant improvement in inter-copulatory efficiency and copulatory efficiency in male rat models ( Aldawsari et al, 2021 ). A previous study also explored the spray drying technology to prepare amorphous solid dispersion of tadalafil, another PDE5 completive inhibitor, using Kollidon® VA64, Koliphore 188, and Kollidon® 30 polymers to improve the ED ( Ahmed et al, 2022 ).…”