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Drug loading mechanism of hollow hydroxyapatite microcapsules

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Inorganic hydroxyapatite microcapsules represent an innovative platform for oral drug delivery, designed as novel excipients known as Template Inverted Particles (TIP). These microcapsules support the development of orally disintegrating tablets (ODTs). This study evaluated their drug-loading capabilities using 11 clinically relevant drugs from all BCS classes, with a particular focus on midazolam HCl, ivermectin, ibuprofen, and metronidazole benzoate. Remarkably, all tested drugs demonstrated a high loading capacity of up to 45% (v/v). When compacted, the drug-loaded TIPs formed mechanically robust tablets, reaching tensile strengths of up to 6 MPa, and disintegrated within seconds upon water contact. The enhanced dissolution rate of the encapsulated drugs is attributed to the high specific surface area of the TIPs and, for certain compounds, the prevention of crystallization due to spatial confinement within the microcapsules. Drug incorporation into the TIPs’ internal hollow cavity is achieved through a self-loading mechanism, eliminating the need for complex, drug-specific loading processes. A mathematical model was developed to describe this self-loading behavior, which ensures targeted deposition of the drug within the particle cavities. Overall, TIP technology offers a versatile, cost-efficient solution with significant potential to streamline the formulation of patient-friendly oral medicines.
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Drug loading mechanism of hollow hydroxyapatite microcapsules
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