International Journal of Pharmaceutics 388 (2010) 159–167 Contents lists available at ScienceDirect International Journal of Pharmaceutics journal homepage: www.elsevier.com/locate/ijpharm Pharmaceutical Nanotechnology Novel multifunctional pharmaceutical excipients derived from microcrystalline cellulose–starch microparticulate composites prepared by compatibilized reactive polymer blending Philip F. Builders a,∗ , Agbo M. Bonaventure a , Adelakun Tiwalade b , Larry C. Okpako c , Anthony A. Attama d a Department of Pharmaceutical Technology and Raw Materials Development, National Institute for Pharmaceutical Research and Development, Abuja, Nigeria b Department of Medicinal Chemistry and Quality Control, National Institute for Pharmaceutical Research and Development, Abuja, Nigeria c School of Pharmacy, University of Bradford, Bradford, United Kingdom d Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria article info Article history: Received 15 October 2009 Received in revised form 22 December 2009 Accepted 24 December 2009 Available online 8 January 2010 Keywords: Microcrystalline cellulose Maize starch Microcrystalline cellulose–maize starch composites Direct compression abstract The choice of excipients remains a critical factor in pharmaceutical formulations. Microcrystalline cellulose–maize starch composites (MCC–Mst) have been prepared by mixing colloidal dispersions of microcrystalline cellulose (MCC) with 10% (w/w) of chemically gelatinized maize starch (Mst) at controlled temperature conditions for use as multifunctional excipients with direct compression and enhanced disintegration abilities. The novel excipient was evaluated for its direct compression and enhanced disintegrant properties and the result compared with the properties of the individual compo- nents. Some of its physicochemical and thermal properties were also determined together with effects of freeze–thaw cycles of processing on the functional and physicochemical properties. The scanning electron micrograph (SEM) shows that the particles of the MCC–Mst were irregular in shape and multiparticulate with a marked degree of asperity. The indirect assessment of the powder flow properties as determined by Carr’s compressibility index and angle of repose showed that the MCC–Mst possesses better flow com- pared with MCC and Mst. MCC–Mst is moderately hygroscopic and shows a Type III moisture sorption isotherm. The FT-IR spectra and DSC thermograms of the composite were different from those of MCC and Mst. The hardness of aspirin tablets was enhanced by incorporating MCC–Mst and MCC, but was reduced by Mst. While the tablets prepared with MCC–Mst and Mst disintegrated within 7 min, aspirin compacts devoid of any excipient and those prepared with MCC did not disintegrate even after 2 h. Acetaminophen compacts prepared with MCC and MCC–Mst showed similar compact hardness characteristics and load- ing properties. The loading capacity of the different samples of the composite decreased with increase in the freeze–thaw cycles. The loading capacity of the different materials as assessed by their compact hard- ness efficiency can be represented as follows (MCC > T0 > T1 > T4 > T3 > T2 > Mst). Generally, the different samples of MCC–Mst are characterized by physicochemical and functional properties that are similar at different degrees to MCC and Mst. © 2010 Elsevier B.V. All rights reserved. 1. Introduction Numerous medical conditions abound which requires the drug to be swallowed whole and the medicament released rapidly in the gastrointestinal tract (GIT) (Newman et al., 2008). In the devel- opment of such important delivery system, one shortcut is the use of high-performing excipients (Deorkar and Baker, 2008). The choice of excipients becomes critical in terms of its functionality as regards direct compression and rapid disintegration abilities (Zhao ∗ Corresponding author. Tel.: +234 8035874698. E-mail address: philsonsky@yahoo.com (P.F. Builders). and Augsburger, 2005; Chang and Chang, 2007). Only few polymers posses multiple functionalities especially in terms of good flow, direct compression and enhanced disintegration abilities. Thus, novel polymer biomaterials with effective multifunctional proper- ties are continually being sought for drug delivery purposes (York, 1992; Watering et al., 2005). The importance of good powder flow and simplicity of direct compression technology as well as the ben- efits of efficient disintegrants in the formulation of rapid release tablets cannot be over emphasized. Many pharmaceutical scientists have focused their attention on the production of multifunctional excipients with enhanced performance to meet the needs of formu- lation experts in terms of costs of production, enhanced excipient functionality and quality of tablets (Chang and Chang, 2007). 0378-5173/$ – see front matter © 2010 Elsevier B.V. All rights reserved. doi:10.1016/j.ijpharm.2009.12.056