A drug-carrying microsphere-microneedle array for controllable drug administration, a preparation method therefor, and application thereof. The method comprises: preparing drug-carrying microspheres with a uniform particle size on the basis of a microfluidic technique, placing the drug-carrying microspheres into a pyramid microneedle template filled with a microneedle hydrogel solution, curing same, and then removing the microneedle template to obtain a drug-carrying microsphere-microneedle array. In the prepared drug-carrying microsphere-microneedle array, the drug-carrying microspheres have good sphericity, a good drug release rate and uniformly fill each needle tip, and a microneedle punctures into the skin to assist in the uniform subcutaneous distribution of the drug-carrying microspheres, thereby achieving the aim of controllable transdermal drug administration. The drug-carrying microsphere-microneedle array for controllable drug administration has the advantages of good drug controllability, a low preparation cost, easy operation, etc., has high practicability, and is suitable for popularization.
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