RETRACTED: Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route (Retracted Article)

被引:5
作者
Ahmed, Osama A. A. [1 ,2 ]
Fahmy, Usama A. [1 ]
Badr-Eldin, Shaimaa M. [1 ,3 ]
Aldawsari, Hibah M. [1 ]
Awan, Zuhier A. [4 ]
Asfour, Hani Z. [5 ]
Kammoun, Ahmed K. [6 ]
Caruso, Giuseppe [7 ]
Caraci, Filippo [7 ,8 ]
Alfarsi, Anas [1 ]
Al-Ghamdi, Raniyah A. [9 ]
Al-Ghamdi, Rawan A. [10 ]
Alhakamy, Nabil A. [1 ,2 ,11 ]
机构
[1] King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut, Jeddah 21589, Saudi Arabia
[2] King Abdulaziz Univ, Fac Pharm, Adv Drug Delivery Res Grp, Jeddah 21589, Saudi Arabia
[3] Cairo Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo 11562, Egypt
[4] King Abdulaziz Univ, Fac Med, Dept Clin Biochem, Jeddah 21589, Saudi Arabia
[5] King Abdulaziz Univ, Fac Med, Dept Med Microbiol & Parasitol, Jeddah 21589, Saudi Arabia
[6] King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut Chem, Jeddah 21589, Saudi Arabia
[7] Oasi Res Inst IRCCS, Via Conte Ruggero 73, I-94018 Troina, EN, Italy
[8] Univ Catania, Dept Drug Sci, I-95125 Catania, Italy
[9] Ibn Sina Natl Coll Med Studies, Clin Pharm Dept, Jeddah 22421, Saudi Arabia
[10] Ibn Sina Natl Coll Med Studies, Jeddah 22421, Saudi Arabia
[11] King Abdulaziz Univ, Ctr Excellence Drug Res & Pharmaceut Ind, Jeddah 21589, Saudi Arabia
关键词
flibanserin; transfersomes; hydrogel; ex vivo permeation; in vivo pharmacokinetics; IN-SITU GEL; TRANSDERMAL DELIVERY; SEXUAL DYSFUNCTION; DRUG-RELEASE; VIVO; DESIGN; NANOPARTICLES; VESICLES; VITRO; BIOAVAILABILITY;
D O I
10.3390/nano10071270
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Flibanserin (FLB) is a nonhormonal medicine approved by the Food and Drug Administration (FDA) to treat the hypoactive sexual appetite disorder in females. However, the peroral administration of the medicine is greatly affected by its poor bioavailability as a result of its extensive first-pass effect and poor solubility. Aiming at circumventing these drawbacks, this work involves the formulation of optimized FLB transfersome (TRF) loaded intranasal hydrogel. Box-Behnken design was utilized for the improvement of FLB TRFs with decreased size. The FLB-to-phospholipid molar ratio, the edge activator hydrophilic lipophilic balance, and the pH of the hydration medium all exhibited significant effects on the TRF size. The optimized/developed TRFs were unilamellar in shape. Hydroxypropyl methyl cellulose based hydrogel filled with the optimized FLB TRFs exhibited an improved ex vivo permeation when compared with the control FLB-loaded hydrogel. In addition, the optimized TRF-loaded hydrogel exhibited higher bioavailability and enhanced brain delivery relative to the control hydrogel following intranasal administration in Wistar rats. The results foreshadow the possible potential application of the proposed intranasal optimized FLB-TRF-loaded hydrogel to increase the bioavailability and nose-to-brain delivery of the drug.
引用
收藏
页码:1 / 15
页数:14
相关论文
共 50 条
[1]   Nanotransfersomes of carvedilol for intranasal delivery: formulation, characterization and in vivo evaluation [J].
Aboud, Heba M. ;
Ali, Adel Ahmed ;
El-Menshawe, Shahira F. ;
Abd Elbary, Ahmed .
DRUG DELIVERY, 2016, 23 (07) :2471-2481
[2]   Self-assembled biodegradable polymeric micelles to improve dapoxetine delivery across the blood-brain barrier [J].
Abourehab, Mohammed A. S. ;
Ahmed, Osama A. A. ;
Balata, Gehan F. ;
Almalki, Waleed H. .
INTERNATIONAL JOURNAL OF NANOMEDICINE, 2018, 13 :3679-3687
[3]   Hydrogel: Preparation, characterization, and applications: A review [J].
Ahmed, Enas M. .
JOURNAL OF ADVANCED RESEARCH, 2015, 6 (02) :105-121
[4]   In situ misemgel as a multifunctional dual-absorption platform for nasal delivery of raloxifene hydrochloride: formulation, characterization, and in vivo performance [J].
Ahmed, Osama A. A. ;
Badr-Eldin, Shaimaa M. .
INTERNATIONAL JOURNAL OF NANOMEDICINE, 2018, 13 :6325-6335
[5]   Investigation of in vivo potential of scorpion venom against skin tumorigenesis in mice via targeting markers associated with cancer development [J].
Al Asmari, Abdulrahman K. ;
Khan, Abdul Quaiyoom .
DRUG DESIGN DEVELOPMENT AND THERAPY, 2016, 10 :3387-3397
[6]   Intranasal drug delivery of didanosine-loaded chitosan nanoparticles for brain targeting; an attractive route against infections caused by aids viruses [J].
Al-Ghananeem, Abeer M. ;
Saeed, Hayder ;
Florence, Rebecca ;
Yokel, Robert A. ;
Malkawi, Ahmad H. .
JOURNAL OF DRUG TARGETING, 2010, 18 (05) :381-388
[7]   Acute and Repeated Flibanserin Administration in Female Rats Modulates Monoamines Differentially Across Brain Areas: A Microdialysis Study [J].
Allers, Kelly A. ;
Dremencov, Eliyahu ;
Ceci, Angelo ;
Flik, Gunnar ;
Ferger, Boris ;
Cremers, Thomas I. F. H. ;
Ittrich, Carina ;
Sommer, Bernd .
JOURNAL OF SEXUAL MEDICINE, 2010, 7 (05) :1757-1767
[8]   Optimized nano-transfersomal films for enhanced sildenafil citrate transdermal delivery: ex vivo and in vivo evaluation [J].
Badr-Eldin, Shaimaa M. ;
Ahmed, Osamaa A. A. .
DRUG DESIGN DEVELOPMENT AND THERAPY, 2016, 10 :1323-1333
[9]  
Borsini F, 2004, US Patent App., Patent No. [10/882, 10882]
[10]   Overview of natural hydrogels for regenerative medicine applications [J].
Catoira, Marta Calvo ;
Fusaro, Luca ;
Di Francesco, Dalila ;
Ramella, Martina ;
Boccafoschi, Francesca .
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE, 2019, 30 (10)