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Alfuzosin hydrochloride-loaded low-density gastroretentive sponges: development, in vitro characterization and gastroretentive monitoring in healthy volunteers via MRI.
Pharm Dev Technol. 2020 Jun; 25(5):566-578.PD

Abstract

The current work aimed to develop low-density gastroretentive sponges loaded with alfuzosin HCl (ALF) to sustain the rate of drug release, improve its oral bioavailability and deliver it to the main site of absorption. Sponges were developed, according to a 23 full factorial design, by compression of the lyophilized ALF-loaded hydroxypropylmethylcellulose (HPMC) or chitosan (CH) solutions. The influences of the polymer type, grade and concentration on the appearance, topography, porosity, density, in vitro ALF release, floating behavior, swelling, erosion, and mucoadhesive potential of the developed sponges were explored. Based on the desirability value, the best achieved system was selected. The gastroretentive potential of this system was evaluated in healthy male volunteers via MRI. Soft and flexible sponges were developed. They were characterized with interconnecting pores and channels and had excellent floating properties with respect to floating lag time and duration. Compared to HPMC-based sponges, CH-based ones exhibited higher porosity, larger pore diameters, lower bulk densities, higher drug release rates, larger swelling ratios, faster erosion rates and better mucoadhesive properties. MRI of magnetite-loaded best-achieved CH-based system (F8) ascertained the development of a promising gastroretentive system; exhibiting a gastric residence period of at least 5 h.

Authors+Show Affiliations

Department of Pharmaceutics, National Organization for Drug Control and Research, Giza, Egypt.Department of Pharmaceutics, National Organization for Drug Control and Research, Giza, Egypt.Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31967910

Citation

Abd El-Aziz, Marwa Farrag, et al. "Alfuzosin Hydrochloride-loaded Low-density Gastroretentive Sponges: Development, in Vitro Characterization and Gastroretentive Monitoring in Healthy Volunteers Via MRI." Pharmaceutical Development and Technology, vol. 25, no. 5, 2020, pp. 566-578.
Abd El-Aziz MF, Ismail S, Tadros MI, et al. Alfuzosin hydrochloride-loaded low-density gastroretentive sponges: development, in vitro characterization and gastroretentive monitoring in healthy volunteers via MRI. Pharm Dev Technol. 2020;25(5):566-578.
Abd El-Aziz, M. F., Ismail, S., Tadros, M. I., & Elnabarawi, M. A. (2020). Alfuzosin hydrochloride-loaded low-density gastroretentive sponges: development, in vitro characterization and gastroretentive monitoring in healthy volunteers via MRI. Pharmaceutical Development and Technology, 25(5), 566-578. https://doi.org/10.1080/10837450.2020.1720235
Abd El-Aziz MF, et al. Alfuzosin Hydrochloride-loaded Low-density Gastroretentive Sponges: Development, in Vitro Characterization and Gastroretentive Monitoring in Healthy Volunteers Via MRI. Pharm Dev Technol. 2020;25(5):566-578. PubMed PMID: 31967910.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Alfuzosin hydrochloride-loaded low-density gastroretentive sponges: development, in vitro characterization and gastroretentive monitoring in healthy volunteers via MRI. AU - Abd El-Aziz,Marwa Farrag, AU - Ismail,Soha, AU - Tadros,Mina Ibrahim, AU - Elnabarawi,Mohamed Ahmed, Y1 - 2020/02/06/ PY - 2020/1/23/pubmed PY - 2020/1/23/medline PY - 2020/1/23/entrez KW - Alfuzosin hydrochloride KW - gastroretentive potential KW - low-density KW - magnetic resonance imaging KW - magnetite-loaded sponges SP - 566 EP - 578 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 25 IS - 5 N2 - The current work aimed to develop low-density gastroretentive sponges loaded with alfuzosin HCl (ALF) to sustain the rate of drug release, improve its oral bioavailability and deliver it to the main site of absorption. Sponges were developed, according to a 23 full factorial design, by compression of the lyophilized ALF-loaded hydroxypropylmethylcellulose (HPMC) or chitosan (CH) solutions. The influences of the polymer type, grade and concentration on the appearance, topography, porosity, density, in vitro ALF release, floating behavior, swelling, erosion, and mucoadhesive potential of the developed sponges were explored. Based on the desirability value, the best achieved system was selected. The gastroretentive potential of this system was evaluated in healthy male volunteers via MRI. Soft and flexible sponges were developed. They were characterized with interconnecting pores and channels and had excellent floating properties with respect to floating lag time and duration. Compared to HPMC-based sponges, CH-based ones exhibited higher porosity, larger pore diameters, lower bulk densities, higher drug release rates, larger swelling ratios, faster erosion rates and better mucoadhesive properties. MRI of magnetite-loaded best-achieved CH-based system (F8) ascertained the development of a promising gastroretentive system; exhibiting a gastric residence period of at least 5 h. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/31967910/Alfuzosin_hydrochloride-loaded_low-density_gastroretentive_sponges:_development,_in_vitro_characterization_and_gastroretentive_monitoring_in_healthy_volunteers_via_MRI L2 - http://www.tandfonline.com/doi/full/10.1080/10837450.2020.1720235 DB - PRIME DP - Unbound Medicine ER -
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