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Enhancement of Dissolution and Skin Permeability of Pentazocine by Proniosomes and Niosomal Gel

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Abstract

Proniosomes (PN) are the dry water-soluble carrier systems that may enhance the oral bioavailability, stability, and topical permeability of therapeutic agents. The low solubility and low oral bioavailability due to extensive first pass metabolism make Pentazocine as an ideal candidate for oral and topical sustained release delivery. The present study was aimed to formulate the PNs by quick slurry method that are converted to niosomes (liquid dispersion) by hydration, and subsequently formulated to semisolid niosomal gel. The PNs were found in spherical shape in the SEM and stable in the physicochemical and thermal analysis (FTIR, TGA, and XRD). The quick slurry method produced high recovery (> 80% yield) and better flow properties (θ = 28.1–37.4°). After hydration, the niosomes exhibited desirable entrapment efficiency (44.45–76.23%), size (4.98–21.3 μm), and zeta potential (− 9.81 to − 21.53 mV). The in vitro drug release (T100%) was extended to more than three half-lives (2–4 h) and showed good fit to Fickian diffusion indicated by Korsmeyer-Peppas model (n = 0.136–0.365 and R2 = 0.9747–0.9954). The permeation of niosomal gel was significantly enhanced across rabbit skin compared to the pure drug-derived gel. Therefore, the PNs are found promising candidates for oral as dissolution enhancement and sustained release for oral and topical delivery of pentazocine for the management of cancer pain.

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Authors and Affiliations

  1. Department of Pharmacy, The Islamia University of Bahawalpur, Railway Road, Bahawalpur, Punjab, 63100, Pakistan

    Asadullah Madni, Muhammad Abdur Rahim, Muhammad Ahmad Mahmood, Abdul Jabar, Hassan Shah & Arshad Khan

  2. Department of Pharmacy, University of Lahore-Gujrat Campus, Gujrat, 50700, Punjab, Pakistan

    Mubashar Rehman

  3. College of Pharmacy, University of Sargodha, Sargodha, 40100, Punjab, Pakistan

    Nayab Tahir

  4. Department of Pharmacy, COMSATS Institute of Science and Technology, Abbottabad, Khyber Pakhtunkhwa, 22010, Pakistan

    Aamna Shah

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  1. Asadullah Madni
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Madni, A., Rahim, M.A., Mahmood, M.A. et al. Enhancement of Dissolution and Skin Permeability of Pentazocine by Proniosomes and Niosomal Gel. AAPS PharmSciTech 19, 1544–1553 (2018). https://doi.org/10.1208/s12249-018-0967-6

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