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Planta Med 2019; 85(03): 249-257
DOI: 10.1055/a-0759-2208
Pharmacokinetic Investigations
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Increased Oral Bioavailability of Piperine from an Optimized Piper nigrum Nanosuspension

Fatiqa Zafar
1   Department of Chemistry, University of Agriculture, Faisalabad, Pakistan
,
Nazish Jahan
1   Department of Chemistry, University of Agriculture, Faisalabad, Pakistan
,
Khalil-Ur-Rahman,
Haq Nawaz Bhatti
1   Department of Chemistry, University of Agriculture, Faisalabad, Pakistan
› Author Affiliations
Further Information

Publication History

received 11 May 2018
revised 29 September 2018

accepted 09 October 2018

Publication Date:
24 October 2018 (online)

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Abstract

The aim of the present study was to enhance the pharmaceutical potential and oral bioavailability of piperine, which is the bioactive constituent of Piper nigrum, using the nanosuspension approach. Nanoprecipitation, which is a simple and reproducible process, was used for nanosuspension formulation. To prepare a pharmaceutical-grade nanosuspension with the required particle size, important formulation parameters (amount of plant extract, concentration of stabilizer, and antisolvent-to-solvent ratio) were optimized using the central composite design of response surface methodology. The optimized nanosuspension was characterized using scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, and in vitro dissolution testing as well as by measuring the zeta potential. In vivo pharmacokinetic studies were conducted to determine the bioavailability of the prepared nanosuspension. Results of the optimization study indicated that 0.13% plant extract, 0.25% stabilizer, and an antisolvent-to-solvent ratio of 10.0 were the best parameters to obtain a homogeneous nanosuspension with the required particle size. The optimized nanosuspension demonstrated a mean particle size, polydispersity index, and zeta potential of 172.5 nm, 0.241, and − 16.6 mV, respectively. The results of the characterization studies illustrated that the nanosuspension was in the nanometer size range and had good surface morphology. The optimized nanosuspension showed a better dissolution rate and a 3.65-fold higher oral bioavailability for the P. nigrum nanosuspension than its coarse suspension. The present outcomes clearly demonstrated that to obtain an effective therapeutic potential, nanoformulation of medicinal plants is a better alternative than conventional dosage forms.

Key words

nanosuspension - bioavailability - piperine - pharmacokinetics - Piper nigrum - Piperaceae

Supporting Information

    FTIR spectra of the P. nigrum coarse plant extract, P. nigrum nanosuspension, and stabilizer (HPMC), HPLC chromatograms of the P. nigrum coarse plant extract, P. nigrum nanosuspension (at Cmax) and piperine standard, and experimental conditions used in the optimization study are provided as Supporting Information.

  • Supporting Information
 

  • References

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