PMID- 34685271
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20211026
IS  - 2073-4360 (Electronic)
IS  - 2073-4360 (Linking)
VI  - 13
IP  - 20
DP  - 2021 Oct 13
TI  - Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with 
      Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual 
      Behavior Studies in Male Rats.
LID - 10.3390/polym13203512 [doi]
LID - 3512
AB  - Sildenafil citrate (SLC) is a frequently used medication (Viagra(R)) 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(R) P188, Kollidon(R) 30, and Kollidon(R)-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(R)-VA64 could be 
      regarded as a potential strategy for improving the solubility, in vitro 
      dissolution, and therapeutic efficacy of SLC.
FAU - Aldawsari, Mohammed F
AU  - Aldawsari MF
AUID- ORCID: 0000-0003-1298-4863
AD  - Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz 
      University, Alkharj 11942, Saudi Arabia.
FAU - Anwer, Md Khalid
AU  - Anwer MK
AUID- ORCID: 0000-0002-5227-3954
AD  - Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz 
      University, Alkharj 11942, Saudi Arabia.
FAU - Ahmed, Mohammed Muqtader
AU  - Ahmed MM
AUID- ORCID: 0000-0001-6911-0652
AD  - Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz 
      University, Alkharj 11942, Saudi Arabia.
FAU - Fatima, Farhat
AU  - Fatima F
AD  - Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz 
      University, Alkharj 11942, Saudi Arabia.
FAU - Soliman, Gamal A
AU  - Soliman GA
AUID- ORCID: 0000-0003-4622-3501
AD  - Department of Pharmacology, College of Pharmacy, Prince Sattam Bin Abdulaziz 
      University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia.
AD  - Department of Pharmacology, College of Veterinary Medicine, Cairo University, 
      Giza 12211, Egypt.
FAU - Bhatia, Saurabh
AU  - Bhatia S
AD  - Natural and Medical Sciences Research Center, University of Nizwa, Birkat Al Mauz 
      616, Nizwa P.O. Box 33, Oman.
AD  - School of Health Science, University of Petroleum and Energy Studies, Dehradun 
      248007, Uttarakhand, India.
FAU - Zafar, Ameeduzzafar
AU  - Zafar A
AD  - Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, 
      Aljouf Region, Saudi Arabia.
FAU - Aboudzadeh, M Ali
AU  - Aboudzadeh MA
AUID- ORCID: 0000-0001-8829-8072
AD  - Institut des Sciences Analytiques et de Physico-Chimie pour l'Environnement et 
      les Materiaux, IPREM, UMR5254, CNRS, University Pau & Pays Adour, E2S UPPA, 64000 
      Pau, France.
LA  - eng
PT  - Journal Article
DEP - 20211013
PL  - Switzerland
TA  - Polymers (Basel)
JT  - Polymers
JID - 101545357
PMC - PMC8536963
OTO - NOTNLM
OT  - Kollidon(R) 30
OT  - Kollidon(R)-VA64
OT  - Kolliphor(R) P188
OT  - erectile dysfunction
OT  - polymer
OT  - sildenafil citrate
COIS- The authors declare no conflict of interest.
EDAT- 2021/10/24 06:00
MHDA- 2021/10/24 06:01
PMCR- 2021/10/13
CRDT- 2021/10/23 01:21
PHST- 2021/09/03 00:00 [received]
PHST- 2021/10/07 00:00 [revised]
PHST- 2021/10/11 00:00 [accepted]
PHST- 2021/10/23 01:21 [entrez]
PHST- 2021/10/24 06:00 [pubmed]
PHST- 2021/10/24 06:01 [medline]
PHST- 2021/10/13 00:00 [pmc-release]
AID - polym13203512 [pii]
AID - polymers-13-03512 [pii]
AID - 10.3390/polym13203512 [doi]
PST - epublish
SO  - Polymers (Basel). 2021 Oct 13;13(20):3512. doi: 10.3390/polym13203512.