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Proniosomal Oral Tablets for Controlled Delivery and Enhanced Pharmacokinetic Properties of Acemetacin

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Abstract

Free-flowing proniosomal powders of acemetacin (AC) were prepared using the slurry method and maltodextrin as carrier. Positively charged proniosomes composed of 70:20:10 of Span 60/cholesterol (Chol)/stearylamine (SA), respectively, were successively compressed into tablets using direct compression method. The tablets were characterized for weight variability, friability, hardness, drug content uniformity, and dissolution properties. The in vivo evaluation of the prepared proniosomes (powder or tablet forms) after oral administration was investigated by the determination of AC and its active metabolite indomethacin (IND) in the blood of albino rabbits. Results indicated that the increase of Chol from 10% to 20% markedly reduced the efflux of the drug. Further Chol addition from 30% to 50% led to increased AC release rates. The proniosome tablets of AC showed greater hardness and disintegration time and less friability than AC plain tablets. The dissolution of proniosomal tablets indicated a lower drug release percentage compared to powdered proniosomes and AC plain tablets. The mean pharmacokinetic parameters of AC and IND from different formulations indicated increased t 1/2 and area under the curve (AUC) of both AC and IND for proniosomal tablets compared with both proniosomal powders and AC plain tablets. This study suggested the formulation of AC proniosomal powder into tablets to control and extend its pharmacologic effects.

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Authors and Affiliations

  1. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt

    Tamer M. Shehata, Marwa H. Abdallah & Mahmoud Mokhtar Ibrahim

  2. Department of Pharmaceutical Sciences, Faculty of Clinical Pharmacy, King Faisal University, Al Hassa, Kingdom of Saudi Arabia

    Tamer M. Shehata

  3. Department of Pharmaceutics, Faculty of Pharmacy, Najran University, Najran, Kingdom of Saudi Arabia

    Mahmoud Mokhtar Ibrahim

Authors
  1. Tamer M. Shehata
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  2. Marwa H. Abdallah
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  3. Mahmoud Mokhtar Ibrahim
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Correspondence to Mahmoud Mokhtar Ibrahim.

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Shehata, T.M., Abdallah, M.H. & Ibrahim, M.M. Proniosomal Oral Tablets for Controlled Delivery and Enhanced Pharmacokinetic Properties of Acemetacin. AAPS PharmSciTech 16, 375–383 (2015). https://doi.org/10.1208/s12249-014-0233-5

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