title: Physicomechanical characterization and optimization of EDTA-mPEG and Avicel®-EDTA-mPEG in situ melt dispersion mini-pellets.
abstract: The purpose of this study was to develop a physicomechanically customizable oral metal chelatory in situ hot melt dispersion mini-pellet entity which could be utilized within a binary drug delivery system. Avicel(®) RC/CL type R-591 was included within the in situ hot melt dispersion mini-pellet formulations to determine the physicomechanical effect this compound would have on the mini-pellet formulations. The physicomechanical properties of the hot melt in situ mini-pellet formulations were mathematically fitting to regression curves. Physicomechanical adjustment of the in situ hot melt dispersion mini-pellet formulations could be mathematically predicted with the derived regression curve equations. The addition of Avicel(®) RC/CL type R-591 increased the physicomechanical properties such as matrix hardness and increased total disintegration of the in situ hot melt dispersion mini-pellet formulations. The utilization of a physicomechanically customizable oral metal chelatory in situ hot melt dispersion mini-pellet entity within a binary drug delivery system would to achieve a synergistically enhance the activity of a drug-carrying entity or a permeation enhancing entity within a single drug delivery unit. The experimental results indicated that weights of the pellets that achieved optimal hardness ranged between 35 and 45 mg. The melt-dispersion formulations disintegrated within shorter time periods and maintained higher ethylenediaminetetraacetic acid (EDTA) concentrations whereas melt-dispersion formulations which included Avicel(®) had superior physicomechanical properties. Disintegration times ranged between 1,000 s for melt-dispersions containing EDTA and methyloxy polyethylene glycol 2000 (mPEG) only, to >6,000 s for melt-dispersions comprising EDTA, mPEG, and Avicel(®).
authors.affiliation: Faculty of Health Sciences, Department of Pharmacy and Pharmacology, University of the Witwatersrand, 7 York Road, Parktown, 2193, Johannesburg, South Africa.
authors.forename: Angus R
authors.initials: AR
authors.lastname: Hibbins
authors.forename: Yahya E
authors.initials: YE
authors.lastname: Choonara
authors.forename: Pradeep
authors.initials: P
authors.lastname: Kumar
authors.forename: Lisa C
authors.initials: LC
authors.lastname: du Toit
authors.forename: Viness
authors.initials: V
authors.lastname: Pillay
mesh_terms: D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000737:chemistry*; D002614:Chelating Agents / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems; D004492:Edetic Acid / Q000737:chemistry*; D006358:Hot Temperature; D011092:Polyethylene Glycols / Q000737:chemistry*; D011208:Powders
chemical_list: D002614:Chelating Agents; D011208:Powders; D011092:Polyethylene Glycols; D002482:Cellulose; C028210:monomethoxypolyethylene glycol; D004492:Edetic Acid