Abstract
Capsular devices for oral drug delivery were recently proposed and manufactured by injection molding (IM) as an evolution of traditional reservoir systems comprising a core and a functional coating. IM allowed the fabrication of capsule shells with release-controlling features based on the employed materials and the design characteristics. These features are independent of the drug, with significant savings in development time and costs. In previous work, IM was used to produce enteric-soluble capsules from blends of hydroxypropyl methylcellulose acetate succinate, with polyethylene glycol (PEG) as the plasticizer. In this work, the range of plasticizer concentrations and molar mass was broadened to evaluate in-depth how those parameters affect material processability and capsule performance over time. As expected, increasing the amount of the low molar mass plasticizer decreased the viscosity and modulus of the material. This simplified the molding process and enhanced the mechanical resistance of the shell, as observed during assembly. However, some samples turned out translucent, depending on several factors including storage conditions. This was attributed to plasticizer migration issues. Such results indicate that higher molar mass PEGs, while not significantly impacting on processability, lead to capsular devices with consistent performance in the investigated time lapse.
Highlights
Over the last few years, injection molding (IM) has started to be employed in the pharmaceutical field, primarily at the research level for testing its feasibility in the manufacturing of drug products [1].The possibility of producing either immediate-release (IR) dosage forms or drug delivery systems (DDSs) has been evaluated
Hydroxypropyl methylcellulose acetate succinate (HPMCAS, cellulose, 2-hydroxypropyl methyl ether, acetate, hydrogen butanedioate; AQUOT-LG®, Shin-Etsu, Tokyo, Japan) was employed as the main component of the gastroresistant capsule shells in view of its solubility at pH ≥ 5.5, its suitability for hot-processing and the experience acquired on similar IM processes [19,27,28]; polyethylene glycol (PEG; Clariant Masterbatches, Milan, Italy) was chosen as the plasticizer based on previous processing use, and PEG 1500 (PEG1.5; 1400–1600 g/mol), PEG 8000 (PEG8.0; 7300–9000 g/mol) and PEG 20,000 (PEG20; 16,000–25,000 g/mol) were selected in order to evaluate the effect of the molar mass of the plasticizer
hydroxypropyl methylcellulose acetate succinate (HPMCAS)-Based rheological investigation was performedininorder ordertotoassess assessthe theprocessability processabilityof ofHPMCAS, HPMCAS, in TheThe rheological investigation was performed in a process temperature window limited by the need to avoid the degradation of the material that a process temperature window limited by the need to avoid the degradation of the material that would would its application to the manufacturing of drug products
Summary
Over the last few years, injection molding (IM) has started to be employed in the pharmaceutical field, primarily at the research level for testing its feasibility in the manufacturing of drug products [1].The possibility of producing either immediate-release (IR) dosage forms or drug delivery systems (DDSs) has been evaluated. DDSs are able to control the rate, time and/or site of drug release, fulfilling therapeutic needs that could not be met by IR products [2,3,4,5,6,7,8]. The rising interest towards the use of IM in DDS manufacturing derives from the intellectual property associated with the resulting drug products, the flexibility in terms of design and composition, the reduction of both time and costs. Operating conditions, typically involving high pressure and temperature, could reduce microbial contamination on the one hand, and promote drug-polymer interactions on the other. This may lead to the formation of solid solutions increasing the dissolution rate of poorly soluble active ingredients. In order to avoid any degradation phenomena, processing temperatures need to be selected according to the thermal stability of the active molecules contained in the formulation
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