Development of spray-dried amorphous solid dispersions of tadalafil using glycyrrhizin for enhanced dissolution and aphrodisiac activity in male rats

Ahmed, Mohammed Muqtader; Fatima, Farhat; Kalam, Mohd Abul; Alshamsan, Aws; Soliman, Gamal A.; Shaikh, Ahmed Karim; Alshahrani, Saad; Aldawsari, Mohammed F.; Bhatia, Saurabh; Anwer, Md. Khalid

doi:10.1016/j.jsps.2020.11.007

Cited by 19 publications

(15 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The PXRD patterns of pure SLC, SLC-K188, SLC-K30, and SLC-KVA64 are shown in Figure 4 . The PXRD pattern of pure SLC revealed several diffraction peaks between 0 and 60° (2θ), which confirmed the crystalline nature of the drug [ 37 , 41 ]. The solid dispersions SLC-K188 and SLC-K30 showed a few diffraction peaks corresponding to SLC with reduced intensity, indicating partial crystallinity.…”

Section: Resultsmentioning

confidence: 79%

“…The CE (%) and ICE (%) are presented in Figure 7 and Figure 8 . Improvements in CE (81.6%) and ICE (44.9%) were observed when rats were exposed to optimized SLC-KVA64 formulae in comparison to the pure SLC drug [ 37 ]. All observed sexual activity parameters of the optimized SLC-KVA64 were remarkably improved compared to the control and pure SLC drug; these parameters are statistically significant.…”

Section: Resultsmentioning

confidence: 99%

“…Male (250–300 g) and female albino rats (150–200 g) were used for the sexual behavior study [ 37 ]. All animals were bred in the lab care unit at the College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj, Saudi Arabia.…”

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

et al. 2021

Self Cite

View full text Add to dashboard Cite

Sildenafil citrate (SLC) is a frequently used medication (Viagra®) for the treatment of erectile dysfunction (ED). Due to its poor solubility, SLC suffers from a delayed onset of action and poor bioavailability. Hence, the aim of the proposed work was to prepare and evaluate solid dispersions (SDs) with hydrophilic polymers (Kolliphor® P188, Kollidon® 30, and Kollidon®-VA64), in order to enhance the dissolution and efficacy of SLC. The SLC-SDs were prepared using a solvent evaporation method (at the ratio drug/polymer, 1:1, w/w) and characterized by Differential Scanning Calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Scanning electron microscope (SEM), drug content, yield, and in vitro release studies. Based on this evaluation, SDs (SLC-KVA64) were optimized, with a maximum release of drug (99.74%) after 2 h for all the developed formulas. The SDs (SLC-KVA64) were further tested for sexual behavior activity in male rats, and significant enhancements in copulatory efficiency (81.6%) and inter-copulatory efficiency (44.9%) were noted in comparison to the pure SLC drug, when exposed to the optimized SLC-KVA64 formulae. Therefore, SD using Kollidon®-VA64 could be regarded as a potential strategy for improving the solubility, in vitro dissolution, and therapeutic efficacy of SLC.

show abstract

Section: Resultsmentioning

confidence: 79%

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

et al. 2021

Self Cite

View full text Add to dashboard Cite

show abstract

“…The drug can exist in various forms, including crystalline, amorphous, or a combination of both. An amorphous form of the drug relatively has a better dissolution rate and therapeutic effects with reduced doses [30], [31], [32]. Technologies employed in preparing SDs are solvent evaporation, freeze-drying, hot-melt extrusion, and spray drying [33].…”

Section: Of 21mentioning

confidence: 99%

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

Alali¹,

Ahmed²,

Fatima³

et al. 2023

Preprint

View full text Add to dashboard Cite

This study aimed to develop chitosan-based apigenin spray dried solid dispersion using 1:1,1:1.5,1:2 w/w ratios. The results of process yield and drug assay were found to be (87.5%, 94.2%, and 95.86%), (95.2 ±1.34%), (99.5 ±0.85%), and (97.6 ±2.42%), respectively, for AC1, AC2, and AC3. Flow properties indicate the free flow of powders. FTIR revealed compatibility among chitosan and apigenin, and DSC and XRD showed prepared solid dispersion was on a molecular level and available in amorphous. In contrast, SEM images reflect irregular block and near-spherical shape elongated particles in the selected AC2. The antimicrobial examination reflects that AC2 was more effective against Gram-positive, negative, and fungal strains. AC2 SDSDs has more anti-oxidant property compared to pure flavonoid (AGN). Anti-proliferative activity against A549 lung cancer cell lines showed better anti-cancer activity by AC2 SDSDs. The selected AC2 SDSD filled in a 3D shell pill and further characterized for 3D shell pill for dissolution profiles and stability studies. The product has sustained release and similar release profiles after three months of storage. The findings suggest that the AC2 SDSDs may be a promising candidate for further development as a 3D printed drug delivery system for treating multiple disease conditions using model flavonoid- apigenin.

show abstract

“…Mohammed Muqtader Ahmed, et al, prepared amorphous solid dispersion (ASD) of Tadalafil (TDL) by spray-drying, using glycyrrhizin-a natural drug carrier. The optimized formulation showed marked increase in dissolution rate compared to pure TDL 49. Rahul B Chavan et al developed amorphous solid dispersion (ASD) of nisoldipine.…”

mentioning

confidence: 99%

Recent and Relevant Methodology in the Advancement of Solid Dispersion

Talla

Wadher

Umekar

et al. 2021

J. Drug Delivery Ther.

View full text Add to dashboard Cite

Most of the promising drugs in development channels are poorly water-soluble drugs which limit formulation approaches, clinical application because of their low dissolution and bioavailability. And the major current challenges of the pharmaceutical industry are apropos strategies that improve the water solubility of drugs. Solid dispersion has been considered one of the major evolutions in overcoming these issues with several successfully marketed products. Though solid dispersion has been outlined as an efficient drug delivery system, the design of specific dosage forms for pharmaceutical therapy is necessary to improve the solubility and bioavailability of poorly water-soluble drugs. Solid dispersion can be prepared by several methods such as solvent evaporation, melting, and supercritical fluid technology. This review intends to provide an updated overview of the recent trends over the past few years in solid dispersion preparation techniques and polymer used. Along with the various pharmaceutical strategies and future visions for the solubilization of poorly water-soluble drugs Keywords: Solid dispersion, Bioavailability, Solubility, Dissolution parameters, Polymeric carrier

show abstract

Development of spray-dried amorphous solid dispersions of tadalafil using glycyrrhizin for enhanced dissolution and aphrodisiac activity in male rats

Cited by 19 publications

References 33 publications

Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

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

Recent and Relevant Methodology in the Advancement of Solid Dispersion

Contact Info

Product

Resources

About