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Preparation and characterisation of nevirapine oral nanosuspensions.

Raju A, Reddy AJ, Satheesh J, Jithan AV - Indian J Pharm Sci (2014)

Bottom Line: The low solubility of nevirapine can lead to decreased and variable oral bioavailability.The nanosuspension was characterised for particle size, polydispersibility index, crystalline state, particle morphology, in vitro drug release and pharmacokinetics in rats after oral administration.The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Mother Teresa College of Pharmacy, NFC Nagar, RR Dist-501 301, India.

ABSTRACT
The objective of this study was to prepare and characterise nevirapine nanosuspensions so as to improve the dissolution rate of nevirapine. Nevirapine is a nonnucleoside reverse transcriptase inhibitor of immunodeficiency virus type-1 and it is poorly water-soluble antiretroviral drug. The low solubility of nevirapine can lead to decreased and variable oral bioavailability. Nanosuspension can overcome the oral bioavailability problem of nevirapine. Nevirapine nanosuspensions were prepared using nanoedge method. The suspensions were stabilised using surfactants Lutrol F 127 or Poloxamer 407 and hydroxypropyl methyl cellulose. The nanosuspension was characterised for particle size, polydispersibility index, crystalline state, particle morphology, in vitro drug release and pharmacokinetics in rats after oral administration. The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability.

No MeSH data available.


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Mentions: DSC studies were used to characterise the physical state of the drug in various formulations. Thermogram of pure nevirapine and optimised nevirapine nanosuspension using various excipients formulation has shown various peaks at different temperature points. The thermograms are shown in fig. 2. Pure drug has shown a peak at 229°. Nanosuspension prepared using HPMC has shown peak at 226.53° while formulation containing Lutrol F 127 has shown peak at 225.43°. The results suggested no change in melting endotherm, which was present in all the samples tested. There was a slight change in melting temperatures of the drug formulated into nanosuspensions with surfactant and stabiliser but melting endotherm is strong in both the cases and it is stronger than that of the pure drug. Thus, it can be inferred that the drug was not converted either fully or partly into amorphous state upon formulation into nanosuspension in the case of optimised formulation. As the concentration of Lutrol F127 in the formulation might be very low, we did not observe a melting endotherm for this excipient. Saturation solubility was determined for each of the optimised nanosuspensions, pure drug and the marketed formulation. The data is presented in Table 3. From the results we observe that the formulation using Lutrol F 127 has demonstrated higher saturation solubility value compared with marketed suspension. Drug release was studied with optimised formulation and compared with that of the pure drug as well as marketed suspension. The data indicates that the drug release from the optimised formulation was higher when compared with pure drug as well as the marketed suspension (fig. 3). Since there is an increase in the dissolution rate and saturation solubility without any change of physical state to amorphous form, it can be concluded that the enhancement in the dissolution as well as saturation solubility are due to nanonisation and not due to the conversion to a different physical state.


Preparation and characterisation of nevirapine oral nanosuspensions.

Raju A, Reddy AJ, Satheesh J, Jithan AV - Indian J Pharm Sci (2014)

© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4007257&req=5

Mentions: DSC studies were used to characterise the physical state of the drug in various formulations. Thermogram of pure nevirapine and optimised nevirapine nanosuspension using various excipients formulation has shown various peaks at different temperature points. The thermograms are shown in fig. 2. Pure drug has shown a peak at 229°. Nanosuspension prepared using HPMC has shown peak at 226.53° while formulation containing Lutrol F 127 has shown peak at 225.43°. The results suggested no change in melting endotherm, which was present in all the samples tested. There was a slight change in melting temperatures of the drug formulated into nanosuspensions with surfactant and stabiliser but melting endotherm is strong in both the cases and it is stronger than that of the pure drug. Thus, it can be inferred that the drug was not converted either fully or partly into amorphous state upon formulation into nanosuspension in the case of optimised formulation. As the concentration of Lutrol F127 in the formulation might be very low, we did not observe a melting endotherm for this excipient. Saturation solubility was determined for each of the optimised nanosuspensions, pure drug and the marketed formulation. The data is presented in Table 3. From the results we observe that the formulation using Lutrol F 127 has demonstrated higher saturation solubility value compared with marketed suspension. Drug release was studied with optimised formulation and compared with that of the pure drug as well as marketed suspension. The data indicates that the drug release from the optimised formulation was higher when compared with pure drug as well as the marketed suspension (fig. 3). Since there is an increase in the dissolution rate and saturation solubility without any change of physical state to amorphous form, it can be concluded that the enhancement in the dissolution as well as saturation solubility are due to nanonisation and not due to the conversion to a different physical state.

Bottom Line: The low solubility of nevirapine can lead to decreased and variable oral bioavailability.The nanosuspension was characterised for particle size, polydispersibility index, crystalline state, particle morphology, in vitro drug release and pharmacokinetics in rats after oral administration.The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Mother Teresa College of Pharmacy, NFC Nagar, RR Dist-501 301, India.

ABSTRACT
The objective of this study was to prepare and characterise nevirapine nanosuspensions so as to improve the dissolution rate of nevirapine. Nevirapine is a nonnucleoside reverse transcriptase inhibitor of immunodeficiency virus type-1 and it is poorly water-soluble antiretroviral drug. The low solubility of nevirapine can lead to decreased and variable oral bioavailability. Nanosuspension can overcome the oral bioavailability problem of nevirapine. Nevirapine nanosuspensions were prepared using nanoedge method. The suspensions were stabilised using surfactants Lutrol F 127 or Poloxamer 407 and hydroxypropyl methyl cellulose. The nanosuspension was characterised for particle size, polydispersibility index, crystalline state, particle morphology, in vitro drug release and pharmacokinetics in rats after oral administration. The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability.

No MeSH data available.


Related in: MedlinePlus