Disclosed herein are a method for preparation of an inclusion-complex including a physiologically active hydrophobic substance in cyclodextrin and a derivative thereof, and use of the inclusion-complex prepared by the same. More particularly, the present invention provides a method for preparing an inclusion-complex, which includes agitating cyclodextrin and a derivative thereof in an agitator at high speed, spraying a physiologically active hydrophobic substance dissolved in alcohol onto the agitator, and drying and crushing the mixture obtained from the preceding step and, in addition, use of the prepared inclusion-complex. The present inventive method has merits of reduced inclusion time and increased inclusion rate. The prepared inclusion-complex has excellent cell and collagen proliferation effects compared to physiologically active hydrophobic substances which were not inclusion processed, thereby being used in production of a cosmetic composition with improved anti-wrinkle and anti-ageing effects.