Size dependent accumulation of micropaticles particles ranging in size from 1 to 5 μm has been confirmed as an effective strategy for pulmonary targeting in drug delivery system development. However, microparticles from either bottom-up (growth from molecule clusters) or top-down method (grinding from bulk materials) are of high surface energy and tend to form larger aggregates, which may lead to embolization of the pulmary vasculatures, making it an infeasible way for pulmonary drug delivery. In this study, two kinds of micro-sized cocyrstals (baicalein/γCD and asiatic acid/γCD) were prepared for delivering drugs into lungs. The asprepared cocrystals are surface inactive, and can disintegrate and release drug-CD inclution complex, thus avoiding aggregation or Ostwald ripening which are common for tradional microparticles. <i>In vivo</i> biodistribution experiments have demonstrated the intravenously injected micro-cocrystals can efficiently accumulate in lungs without inducing vascular embolization. The pulmonary targeting and therapeutic potential of micro-cocrystals have been further tested in LPS induced mouse model of acute lung injury (ALI). Results have shown the lung-targeted drug delivery can potentially improve the therapeutic effect of treatment. And asiatic acid/γCD reduced pro-inflammatory cytokines more efficiently than asiatic acid alone, baicalein alone and baicalein/γCD, including lung and BALF. In conclusion, micro-cocrystal asiatic acid/γCD was successfully delivered into the lungs by pulmonary administration and it has a significant therapeutic effect on ALI.

Microsized, low surface energy cocrystal for high-efficient pulmonary delivery and acute lung Injury treatment

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