Evaluation of the Impacts of Formulation Variables and Excipients on the Drug Release Dynamics of a Polyamide 6,10-Based Monolithic Matrix Using Mathematical Tools

Abstract

Abstract. Drug release from hydrophilic matrices is regulated mainly by polymeric erosion, disentanglement, dissolution, swelling front movement, drug dissolution and diffusion through the polymeric matrix. These processes depend upon the interaction between the dissolution media, polymeric matrix and drug molecules, which can be significantly influenced by formulation variables and excipients. This study utilized mathematical parameters to evaluate the impacts of selected formulation variables and various excipients on the release performance of hydrophilic polyamide 6,10 (PA 6,10) monolithic matrix. Amitriptyline HCl and theophylline were employed as the high and low solubility model drugs, respectively. The incorporation of different excipient concentrations and changes in formulation components influenced the drug release dynamics as evidenced by computed mathematical quantities (t x% , MDT x%, f 1 , f 2 , k 1 , k 2 , and К F ). The effects of excipients on drug release from the PA 6,10 monolithic matrix was further elucidated using static lattice atomistic simulations wherein the component energy refinements corroborates the in vitro and in silico experimental data. Consequently, the feasibility of modulating release kinetics of drug molecules from the novel PA 6,10 monolithic matrix was well suggested.

Multicomponent Crystals of Amitriptyline as Potential Controlled-Release Systems: Synthesis, Crystal Packing Analysis, and Dissolution Study

“…As seen in Figure 10, the complete dissolution of AMT-HCl in the FaSSGF media occurs in the first 15 min of the experiment. The rapid dissolution of this form agrees with the results in the work of Adeleke et al, 100 given the difference in pH and a larger amount of solute in our work.…”

“…The salt formation approach proposed in the present work is compatible with technological methods for extended-release formulation design that have already been proven to be efficient for AMT-HCl. ,− , The combination of an organic salt (AMT maleate) and polymeric matrices, coatings, or hydrogels would allow the production of ultra-extended controlled-release formulations of AMT with a release time potentially exceeding 24 h and improved patient compliance.…”

In vitro characterization of a synthetic polyamide-based erodible compact disc for extended drug release

“…Polyamide 6,10 was synthesized by interfacial polymerization employing decanedioyldichloride and 1,6-diaminohexane as monomers, cyclohexane/hexane and deionized water as non-polar and polar dispersants respectively and sodium hydroxide as a neutralizing agent (Fig. 1) [34][35][36]. Two solutions were prepared with the aqueous phase containing 1.75 g of 1,6-diaminohexane plus 0.4 g of sodium hydroxide dissolved in 10 mL deionized water while the non-polar phase was composed of 0.2 g decanedioyldichloride evenly dispersed in hexane in cyclohexane (1:4).…”

“…They are constantly in high demand and scientist are seeking additional polymeric carriers for this application [2]. Researchers have documented the attractive clinical application, biocompatibility and potent drug release modulating properties of different aliphatic polyamides [29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44]. Yet, there is still not much information regarding their use as extended release drug carriers.…”