Considering the safety-risk ratio of steroidal contraceptives, the present work was carried out to evaluate ethno-contraceptive use of Cordia dichotoma G. Forst., Boraginaceae, leaves (LCD). Preliminary pharmacological screening was performed on post-coital female albino rats. The leaves extract (LD50 5.50 g/ kg bw) showed 100% anti-implantation activity (n=10) at 800 mg/kg dose level. (2-hydroxypropyl)-β-cyclodextrin (BCD) was used as bioavailability enhancer to form LCD-BCD complex, characterized by DLS, SEM and XRD analyses. The LCD-BCD complex (1:1, w/w) exhibited 100% pregnancy interception (n=20) at the dose level of 250 mg/kg and also showed strong estrogenic potential with a luteal phase defect. Qualitative and quantitative phytochemical analyses were carried out. The LCD extract was standardized by a validated HPTLC method and two contraceptive phytoconstituents, apigenin and luteolin were isolated. A detailed pharmacological analyses followed by chronic toxicity study were performed to predict the reversible nature of the developed phytopharmaceutical. The histological and biochemical estimations detected the reversible contraceptive potential after withdrawal. The observations suggested that the developed phyto-pharmaceutical has potential antifertility activity with safety aspects.