本發明係提供細胞內藥物釋放之組成物及方法。該方法包括：(a)提供一組成物，其包括一治療有效量之藥劑，該藥劑係吸附於具有疏水性表面之中孔徑氫氧基磷灰石(HAP)上；(b)將該組成物暴露至一細胞；(c)使該中孔徑氫氧基磷灰石進入該細胞中並於該細胞之溶酶體中降解，而使該藥劑自該中孔徑氫氧基磷灰石去吸附(desorption)；(d)使該經去吸附之藥劑由該溶酶體釋出至該細胞之細胞質中；以及(e)使該經去吸附之藥劑釋出至細胞外。該組成物包括(a)具疏水性表面之中孔徑氫氧基磷灰石(HAP)；(b)一治療有效量之藥劑，其係吸附於具有疏水性表面之中孔徑氫氧基磷灰石上。該組成物之特徵為：於生體內持續釋放該藥劑達至少4週。Methods and compositions for producing a cellular drug release are disclosed. The method comprises: a) providing a composition comprising a therapeutically effective amount of a pharmacological agent adsorbed onto mesoporous hydroxyapatite (HAP) with hydrophobic surfaces; b) exposing the composition to a cell; c) causing entry of the mesoporous HAP into the cell and degradation of the HAP in the lysosomes of the cell and desorption of the agent from the mesoporous HAP; d) causing release of the desorbed agent from the lysosomes into the cytoplasm of the cell; and e) causing release of the desorbed agent to outside the cell. The composition comprises a) mesoporous HAP with hydrophobic surfaces; and b) a therapeutically effective amount of a pharmacological agent, adsorbed onto the hydrophobic surfaces of the mesoporous HAP. The composition is characterized in that it constantly releases the agentin vivo for a period of at least 4 weeks.
