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Piroxicam/β-cyclodextrin complex included in cellulose derivatives-based matrix microspheres as new solid dispersion-controlled release formulations

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Abstract

New formulations capable to enhance piroxicam (PRX) water solubility and at the same time to control and adjust its release have been developed. For this purpose, two methods have been used and combined to achieve this goal, namely complexation and microencapsulation by O/W emulsion solvent evaporation. In order to modify the drug release, first, microparticles composed of pure PRX and ethylcellulose (EC) or mixtures of EC and hydroxypropylmethylcellulose (HPMC) were prepared, and then, other micropaticles containing the β-cyclodextrin/piroxicam (β-CD/PRX) complex obtained by the solvent evaporation technique and EC or a mixture of EC and HPMC were produced and tested. These formulations were characterized by FT-IR, XRD, optical microscopy, and SEM methods. Drug dissolution tests were carried out in acidic media at pH = 1.2 and 37°C. Depending on the microparticles composition, their size (d10) ranged between 49 μ.m and 121 μ.m and PRXloaded varied from 10.8 % to 27.7 %. The effect of complexation and HPMC polymer on the drug release was investigated; the results demonstrated that the Higuchi’s release constant significantly increased when using the EC/HPMC mixture as a matrix with pure PRX or only EC as a matrix with the β-CD/PRX complex. The results are remarkably promising since the combination of these processes provided new SD-CR formulations of piroxicam which enabled simultaneous enhancement and control of its release from the carriers.

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  1. Laboratory of Advanced Materials and Physical Chemistry for Environment and Health, Faculty of Exact Sciences, Djillali Liabès University of Sidi Bel Abbès, 22000, Algeria

    Oum Elkheir Khoukhi, Zineb El Bahri & Kheira Diaf

  2. Laboratory of Multiphasic and Polymeric Materials, Faculty of Technology, Ferhat Abbas University of Sétif, 19000, Algeria

    Milad Baitiche

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  1. Oum Elkheir Khoukhi
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  2. Zineb El Bahri
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  4. Milad Baitiche
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Correspondence to Zineb El Bahri.

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Khoukhi, O.E., Bahri, Z.E., Diaf, K. et al. Piroxicam/β-cyclodextrin complex included in cellulose derivatives-based matrix microspheres as new solid dispersion-controlled release formulations. Chem. Pap. 70, 828–839 (2016). https://doi.org/10.1515/chempap-2016-0014

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