The present invention discloses a nanoparticulate composition having butylidenephthalide, preparation process and pharmaceutical use thereof. The preparation method of making nanoparticulate composition having butylidenephthalide including contacting butylidenephthalide particles with a least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate composition having butylidenephthalide which having an effective average particle size of less than 2200 nm. It has a potential in stimulating hair growth and with a good aqueous solubility, high stability and bioavailability.本發明揭露一種含有正-丁烯基苯酞的奈米顆粒組合物、製備方法及其用途,所述之製備方法係將一正-丁烯基苯酞與至少一表面穩定劑均勻混合,使表面穩定劑包覆於正-丁烯基苯酞之表面後,生成有效平均粒徑小於約2200奈米之含有正-丁烯基苯酞的奈米顆粒組合物,其不僅水溶性佳、粒徑大小分佈均勻,更能在水中長期穩定,又,具有較高的生物利用度,再者,所述之正-丁烯基苯酞的奈米顆粒組合物更有促進毛髮生長之用途。