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comparative study among different carriers to enhance the bioavailability of aceclofenac via proniosomal system
International Islamic University Malaysia
xix, 184 leaves : colour illustrations ; 30cm.
In the contemporary medical model world, the proniosomal system has served as a new drug delivery system that significantly enhances the bioavailability of drugs with low water solubility. Aceclofenac (ACE), a potent non-steroidal anti-inflammatory drug is used to relieve pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. However, it is characterised by low bioavailability that limited its use. Hence, the application of the proniosomal system can improve the bioavailability of ACE. The present study was intended to develop an optimised proniosomal ACE formula by the use of different carriers. Three formulations of proniosomes were prepared by the slurry method using the 100 mg of ACE, 500 mg of Span 60, 250 mg of cholesterol with 1300 mg of different carriers, i.e., glucose (FN1), maltodextrin (FN2), and mannitol (FN3). The prepared proniosomes were characterised by fourier transform infrared analysis to reveal the compatibility of the drug chosen with the ingredient added. Meanwhile, the powder X-ray diffractometry confirmed the amorphous phase of the prepared proniosomes, and the surfactant layer was observed by scanning electron microscopy. Hydrated proniosomes yielded niosomes with high EE (84%) and 100% drug content. No significant differences (p > 0.05) in entrapment efficiency (EE) of FN1, FN2, and FN3 (82±0.5%, 84±0.66%, and 84±0.34%, respectively) were observed and formulations were used as such for further in vitro and in vivo evaluations. During in vitro drug release studies, the dissolved drug was found to be 42% for the pure drug, while 70%, 17% 30% for FN1, FN2, and FN3 respectively at 15 min. After 24 h, the pure drug showed a maximum of 50 % release while 94%, 80%, 79% drug release were observed after 24 h for FN1, FN2, and FN3, respectively. A comparison between the two methods was made, and the results revealed the appropriateness of the paddle method. The in vivo study conducted using albino rats showed enhanced bioavailability of ACE when glucose and maltodextrin proniosomes were used as a carrier. Maltodextrin proniosomes exhibited fast absorption with 183% relative bioavailability compared to the pure drug, while glucose proniosomes demonstrated 112% relative bioavailability. It was concluded that the proniosomal system enhanced the bioavailability of ACE. The in vitro-in vivo correlation level A successfully built to provide an overview of the predicted drug absorbed from the niosomal dosage form. Nonetheless, the proniosomes prepared were not stable in normal and accelerated conditions after three months. It was suggested that proniosomes should be stored at 4-5 °C, and more studies should be performed on proniosomal storage conditions. HPLC was used for all the required determinations, such as the niosomes EE, drug content, and in vitro and in vivo drug release. Lastly, it was concluded that ACE proniosomes were successfully prepared using different carriers, and maltodextrin proniosomes enhanced ACE bioavailability two-fold in comparison with the pure drug.
"A thesis submitted in partial fulfilment of the requirement for the Degree of Doctor of Philosophy in Pharmaceutical Sciences (Pharmaceutical Technology)."--On title page.
Thesis (Ph.D)--International Islamic University Malaysia, 2020.
Includes bibliographical references (leaves 171-181).