Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film
Benign prostatic hyperplasia (BPH) affects about 90% of men whose ages are over 65. Tadalafil, a selective PDE-5 inhibitor, was approved by FDA for BPH, however, its poor aqueous solubility and bioavailability are considered major drawbacks. This work intended to develop and evaluate oral fast disso...
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| Format: | Article |
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MDPI AG
2023-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/1/173 |
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| author | Kawthar K. Abla Amina T. Mneimneh Ahmed N. Allam Mohammed M. Mehanna |
| author_facet | Kawthar K. Abla Amina T. Mneimneh Ahmed N. Allam Mohammed M. Mehanna |
| author_sort | Kawthar K. Abla |
| collection | DOAJ |
| description | Benign prostatic hyperplasia (BPH) affects about 90% of men whose ages are over 65. Tadalafil, a selective PDE-5 inhibitor, was approved by FDA for BPH, however, its poor aqueous solubility and bioavailability are considered major drawbacks. This work intended to develop and evaluate oral fast dissolving film containing tadalafil-loaded niosomes for those who cannot receive the oral dosage form. Niosomes were statistically optimized by Box-Behnken experimental design and loaded into a polymeric oral film. Niosomes were assessed for their vesicular size, uniformity, and zeta potential. The thickness, content uniformity, folding endurance, tensile strength, disintegration time, and surface morphology were evaluated for the prepared polymeric film. The optimized niosomes revealed high entrapment efficiency (99.78 ± 2.132%) and the film was smooth with good flexibility and convenient thickness (110 ± 10 µm). A fast release of tadalafil was achieved within 5 min significantly faster than the niosomes-free drug film. The in-vivo bioavailability in rats established that the optimized niosomal film enhanced tadalafil systemic absorption, with higher peak concentration (C<sub>max</sub> = 0.63 ± 0.03 µg/mL), shorter T<sub>max</sub> value (0.66-fold), and relative bioavailability of 118.4% compared to the marketed tablet. These results propose that the oral film of tadalafil-loaded niosomes is a suitable therapeutic application that can be passed with ease to geriatric patients who suffer from BPH. |
| first_indexed | 2024-03-09T11:27:54Z |
| format | Article |
| id | doaj.art-c91ec69c65374442a3d6aa9aebea4439 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T11:27:54Z |
| publishDate | 2023-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-c91ec69c65374442a3d6aa9aebea44392023-11-30T23:58:44ZengMDPI AGPharmaceutics1999-49232023-01-0115117310.3390/pharmaceutics15010173Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal FilmKawthar K. Abla0Amina T. Mneimneh1Ahmed N. Allam2Mohammed M. Mehanna3Pharmaceutical Nanotechnology Research Lab, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonPharmaceutical Nanotechnology Research Lab, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonDepartment of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria 21521, EgyptDepartment of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria 21521, EgyptBenign prostatic hyperplasia (BPH) affects about 90% of men whose ages are over 65. Tadalafil, a selective PDE-5 inhibitor, was approved by FDA for BPH, however, its poor aqueous solubility and bioavailability are considered major drawbacks. This work intended to develop and evaluate oral fast dissolving film containing tadalafil-loaded niosomes for those who cannot receive the oral dosage form. Niosomes were statistically optimized by Box-Behnken experimental design and loaded into a polymeric oral film. Niosomes were assessed for their vesicular size, uniformity, and zeta potential. The thickness, content uniformity, folding endurance, tensile strength, disintegration time, and surface morphology were evaluated for the prepared polymeric film. The optimized niosomes revealed high entrapment efficiency (99.78 ± 2.132%) and the film was smooth with good flexibility and convenient thickness (110 ± 10 µm). A fast release of tadalafil was achieved within 5 min significantly faster than the niosomes-free drug film. The in-vivo bioavailability in rats established that the optimized niosomal film enhanced tadalafil systemic absorption, with higher peak concentration (C<sub>max</sub> = 0.63 ± 0.03 µg/mL), shorter T<sub>max</sub> value (0.66-fold), and relative bioavailability of 118.4% compared to the marketed tablet. These results propose that the oral film of tadalafil-loaded niosomes is a suitable therapeutic application that can be passed with ease to geriatric patients who suffer from BPH.https://www.mdpi.com/1999-4923/15/1/173Box-Behnkenmethylcelluloseniosomesoral filmtadalafil |
| spellingShingle | Kawthar K. Abla Amina T. Mneimneh Ahmed N. Allam Mohammed M. Mehanna Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film Pharmaceutics Box-Behnken methylcellulose niosomes oral film tadalafil |
| title | Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film |
| title_full | Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film |
| title_fullStr | Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film |
| title_full_unstemmed | Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film |
| title_short | Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film |
| title_sort | application of box behnken design in the preparation optimization and in vivo pharmacokinetic evaluation of oral tadalafil loaded niosomal film |
| topic | Box-Behnken methylcellulose niosomes oral film tadalafil |
| url | https://www.mdpi.com/1999-4923/15/1/173 |
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