What is it about?
Solid binary systems of nelfinavir with chemically modified cyclodextrin like HP-β-CD were prepared using physical mixtures, kneading, coprecipitation method and freeze-drying techniques in 1:1, 1:2, 1:3 and 1:5 (drug: CD) molar ratios. From the above results, it is possible to conclude that HP- β -CD will able to form true inclusion complexes with nelfinavir at a molar ratio of 1:5 using the freezedrying technique. The dissolution of nelfinavir was markedly enhanced in both systems, showing an initial burst effect of more than 75% in the first 5 min. Hence, the FD system of nelfinavir with HP- β - CD prepared at a molar ratio of 1:5 could be chosen for the formulation of nelfinavir tablets due to the well-documented safety profile of HP- β -CD.
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Why is it important?
Aim of this work was to study the interaction of NFV with the water soluble derivatives of β-CD like HP-β-CD prepared using various methods, in both solution and solid state, so as to develop a soluble form of the drug as a primary step in the development of nelfinavir tablet formulation. Phase solubility technique and UV spectral shift method were used to investigate the interaction of nelfinavir with cyclodextrins in the solution state.
Perspectives
Nelfinavir Mesylate (NFV) is used in the treatment of HIV infection in conjunction with other antiretrovirals.1 Nelfinavir inhibits the HIV viral protease enzyme which prevents cleavage of the gagpol polyprotein, resulting in noninfectious, immature viral particles. Protease inhibitors (PIs) block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. It is practically insoluble in water but well absorbed from oral route. However, due to this disadvantage of poor aqueous solubility this may cause formulation problems and lead to highly variable blood levels, and irreproducible clinical response (therapeutic failure or exaggerated side effects). Therefore, it is important to introduce effective methods to enhance the solubility and dissolution rate of the drug aiming to improve its bioavailability, increase the predictability of the response and/or reduce the dose.
Prof. Ganesh G.R. Godge
P.D.V.V.P.F'S COLLEGE OF PHARMACY AHMEDNAGAR MAHARASHTRA INDIA
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This page is a summary of: Preparation and in vitro Evaluation of Inclusion Complexes of Nelfinavir with Chemically Modified β-cyclodextrins, Dhaka University Journal of Pharmaceutical Sciences, April 2013, Bangladesh Journals Online (BanglaJOL),
DOI: 10.3329/dujps.v11i2.14558.
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