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Development and pharmacokinetic evaluation of spray-dried self-nanoemulsifying drug delivery system of sertraline

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Abstract

The objective of the present study was to develop solid self-nanoemulsifying drug delivery system (SNEDDS) of poorly absorbed drug sertraline (SRT) and evaluation of its pharmacokinetic parameters in rats. The composition of optimized liquid SNEDDS was (25.42 % v/v) Labrafil M 2125 CS and Maisine 35-1 (1:1), (49.72 % v/v) Tween 80 and (24.86 % v/v) Lauroglycol 90 containing 25 mg SRT. Solid SNEDDS was prepared by spray-drying the liquid SNEDDS using dextran 40 as solid carrier. There was no significant difference (p > 0.05) in the droplet size of reconstituted nanoemulsion between both liquid and solid SNEDDS. The surface characterization of spray-dried powder showed a satisfactory regular spherical shape of particles. The internal physical state of SRT was verified by X-ray diffraction analysis indicated the transformation of crystalline structure of SRT to amorphous and molecularly dispersed state. In vitro release of SRT from solid SNEDDS was highly significant (p < 0.01) as compared to unformulated SRT. After oral administration of solid SNEDDS to adult Sprague–Dawley (SD) rats, the area under the curve (AUC) were 2.8- and 6.8-folds and the maximum plasma concentration (Cmax) were 3.5 -and 13-folds higher, respectively compared to those of conventional capsule and unformulated drug suspension. These results reveal that solid SNEDDS results in a significantly increased absorption of SRT compared with that from the marketed conventional capsule and aqueous suspension of SRT. Thus, this solid SNEDDS may provide a useful solid dosage form for oral delivery of poorly-water soluble lipophilic compounds.

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Acknowledgments

One of the authors, Md. A. Rahman is highly grateful to University Grant Commission (UGC) to provide senior research fellowship (SRF). The author is also thankful to Indian Council of Medical Research (ICMR), Gov. of India for approving travel grant to attend “5th BBBB International Conference”, Athens, Greece.

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Authors and Affiliations

  1. Faculty of Pharmacy, Integral University, Kursi Road, Lucknow, 226026, India

    Md. Akhlaquer Rahman & Md. Mujahid

  2. Department of Pharmacognosy, College of Pharmacy, King Khalid University, Abha, Saudi Arabia

    Arshad Hussain

  3. Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India

    Zeenat Iqbal

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  1. Md. Akhlaquer Rahman
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  2. Md. Mujahid
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  3. Arshad Hussain
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  4. Zeenat Iqbal
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Correspondence to Md. Akhlaquer Rahman.

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MA. Rahman, M. Mujahid, A. Hussain, and Z. Iqbal declare that they have no conflict of interest.

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Rahman, M.A., Mujahid, M., Hussain, A. et al. Development and pharmacokinetic evaluation of spray-dried self-nanoemulsifying drug delivery system of sertraline. Journal of Pharmaceutical Investigation 47, 325–333 (2017). https://doi.org/10.1007/s40005-016-0263-y

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  • DOI: https://doi.org/10.1007/s40005-016-0263-y

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