[ Pharmaceutical Sciences Asia - ONLINE ]
E-ISSN 2586-8470
[ Journal Abbreviation: Pharm.Sci.Asia ]
Mahidol University Journal of Pharmaceutical Sciences
  FORMER NAME   "Mahidol University Journal of Pharmaceutical Sciences" Published Since 1974

 
Abstracts

DOI: 10.29090/psa.2019.03.018.0020Pharm Sci Asia 2019; 46(3), 193-205
 

Design and characterisation of lopinavir nanocrystals for solubility and dissolution enhancement

Anilkumar Shinde1* , Namdeo Jadhav1, Harinath More 1, Heena Naikwadi1

- Bharati Vidyapeeth College of Pharmacy, Kolhapur


The objective of present work was to prepare nanocrystals of Lopinavir (LPN) to enhance its solubility and dissolution rate with aim of dose reduction and minimising the side effects associated with it’s oral administration. Nanocrystals of LPN were prepared by anti-solvent precipitation method using a 32 full factorial design, employing stirring speed (X1) and concentration of surfactant (X2) as independent variables. The nanocrystals obtained were characterised mainly for particle size (PS), zeta potential (ZP), crystallinity, saturation solubility, in vitro dissolution and permeability. Results demonstrated profound effect of concentration of surfactant (pluronic F-68) on both the PS and polydispersity index (PDI) values. The optimised nanocrystals formulation had particle size 265nm, PDI 0.260 and ZP in the range of -18.0 to -22.5mv. X-Ray diffraction studies (XRPD) and Differential scanning calorimetry (DSC) studies suggested nanocrystal formation and absence of crystalline peaks, indicating loss of crystallinity, additionally confirmed by scanning electron microscopy (SEM). Nanocrystals showed 30.45 fold enhancements in aqueous solubility, and 38.5 fold in phosphate buffer pH 6.8, as compared to pure LPN. In vitro release studies have demonstrated 92.20% cumulative drug release within 3 hrs from nanocrystals compared to 42.65% from pure LPN. Even, increase in permeation flux from 423.1 μg/cm2/hr to 632.93 μg/cm2/hr in case of nanocrystals was also indication of enhanced dissolution. Stable LPN nanocrystals formulated by anti-solvent precipitation method shows improved solubility and dissolution. It has been concluded that LPN nanocrystals were obtained with significant improvement in saturation solubility and drug losing it’s crystalline nature when compared with plain drug.


Keyword:

Lopinavir; Nanocrystals; antisolvent precipitation;Dissolution




Download full paper (PDF File size: 1,624.76 KB.)





Vol.46
No.4
October - December 2019

See other volume

 


Vol.46
No.3
July - September 2019

See other volume

 


Vol.46
No.2
April - June 2019

See other volume

 


Vol.46
No.1
January - March 2019

See other volume

 
 
 

Home
Aims and Scope
Editorial Board
Publication Ethics
Instruction to Authors
Announcement
All Volumes & Issues
Submit Online
Contact us
   
Search
   
Faculty of Pharmacy Mahidol University
Mahidol University
Member's menu

You're now loging on with following account:
Guest (unknown)

Please Sign in or Register



Pharmaceutical Sciences Asia by Faculty of Pharmacy, Mahidol University, Thailand is licensed under CC BY-NC-ND 4.0

    Copyright © 2017-2024
    Faculty of Pharmacy, Mahidol University, THAILAND
 

We use Cookies

This site uses cookies to personalise your experience and analyse site traffic. By Clicking ACCEPT or continuing to browse the site you are agreeing to our use of cookies.