PMID- 34435939
OWN - NLM
STAT- MEDLINE
DCOM- 20220128
LR  - 20220128
IS  - 1097-9867 (Electronic)
IS  - 1083-7450 (Linking)
VI  - 26
IP  - 9
DP  - 2021 Nov
TI  - Solid self nano-emulsifying system for the enhancement of dissolution and 
      bioavailability of Prasugrel HCl: in vitro and in vivo studies.
PG  - 1021-1033
LID - 10.1080/10837450.2021.1973495 [doi]
AB  - Prasugrel Hydrochloride (PHCl) is an antiplatelet drug. It is a class II drug 
      with variable bioavailability. The objective of this work was to enhance the 
      solubility and hence the bioavailability and efficacy of PHCl. A Self 
      Nano-Emulsifying Drug Delivery System (SNEDDS) was prepared using Kolliphor El, 
      Maisine 35-1, and Transcutol P as surfactant, oil, and co-surfactant, 
      respectively in a ratio 10:72:18 v/v%. The SNEDDS was converted into solid by 
      adsorption onto Neusilin. In vitro release of the drug from SNEDDS in (pH = 4) at 
      37  degrees C and 75 rpm for 45 min was studied. The results were compared to those from 
      the unprocessed PHCl and Lexar((R)) (the commercial drug). In-vivo studies 
      (platelet Aggregation and bleeding time) were conducted using rats as animal 
      models. It was found that the particle size of the SNEDDS ranged between 80 and 
      155 nm and EE% was in the range of 90.2% +/- 0.4. The release from SNEDDS was about 
      84% compared to around 25% from unprocessed PHCl and 65% from Lexar((R)) after 
      15 min. The platelet aggregation of the formula was lower than the PHCl, and 
      Lexar((R)) indicating higher bioavailability. In conclusion, SNEDDS with high EE% 
      was prepared and was successful in enhancing the solubility, dissolution rate, 
      and the bioavailability.
FAU - Khanfar, Mai
AU  - Khanfar M
AD  - Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University 
      of Science and Technology, ‎Irbid‎, Jordan.
FAU - Al-Nimry, Suhair
AU  - Al-Nimry S
AD  - Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University 
      of Science and Technology, ‎Irbid‎, Jordan.
FAU - Attar, Shatha
AU  - Attar S
AD  - Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University 
      of Science and Technology, ‎Irbid‎, Jordan.
LA  - eng
PT  - Journal Article
DEP - 20210905
PL  - England
TA  - Pharm Dev Technol
JT  - Pharmaceutical development and technology
JID - 9610932
RN  - 0 (Emulsifying Agents)
RN  - 0 (Platelet Aggregation Inhibitors)
RN  - G89JQ59I13 (Prasugrel Hydrochloride)
SB  - IM
MH  - Animals
MH  - Biological Availability
MH  - Dose-Response Relationship, Drug
MH  - Emulsifying Agents/blood/*pharmacokinetics
MH  - Male
MH  - Platelet Aggregation Inhibitors/blood/*pharmacokinetics
MH  - Prasugrel Hydrochloride/blood/*pharmacokinetics
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Solubility
MH  - X-Ray Diffraction/methods
OTO - NOTNLM
OT  - Kolliphor
OT  - Maisine
OT  - Prasugrel HCl
OT  - Transcutol
OT  - platelet aggregation
OT  - solid self emulsifying agent
EDAT- 2021/08/27 06:00
MHDA- 2022/01/29 06:00
CRDT- 2021/08/26 12:20
PHST- 2021/08/27 06:00 [pubmed]
PHST- 2022/01/29 06:00 [medline]
PHST- 2021/08/26 12:20 [entrez]
AID - 10.1080/10837450.2021.1973495 [doi]
PST - ppublish
SO  - Pharm Dev Technol. 2021 Nov;26(9):1021-1033. doi: 10.1080/10837450.2021.1973495. 
      Epub 2021 Sep 5.