Nanotechnology has prompted new aspirations for managing modern human challenges. Furthermore, it has been utilized for aid in the prevention, diagnosis, and treatment of ovulatory disorders. Women with ovulatory issues may benefit from formulation using nanotechnology as an alternative possible treatment. Clomiphene citrate is non-steroidal, ovulatory stimulant that acts as a selective estrogen receptor modulator (SERM). It is a triphenyl ethylene stilbene derivative that is primarily used to trigger ovulation in female infertility cases where there is anovulation. Anovulatory infertility is most frequently caused by polycystic ovarian syndrome (PCOS) which is a gynaecological endocrine disorder. Elevated serum concentrations of androgens, LH and insulin are the main features of its endocrine profile. The primary goal of treating PCOS-related infertility is to increase the amount of FSH that is exposed to the ovary, either by antagonizing the estrogenic effects of clomiphene citrate in the hypothalamus or by directly affecting the ovary using recombinant FSH. In about 80% of treated individuals, ovulation is recovered by clomiphene citrate. In this review, we discussed the chemistry and pharmacology of clomiphene citrate as well as the delivery of clomiphene citrate via nanosystems for improving solubility and limiting side effects. The hyphenated techniques for analysing and quantifying clomiphene citrate in solvents and biological samples are also overviewed.