Department of Zoology, Punjab Agricultural University, Ludhiana, India.
School of Chemistry and Biochemistry, Thapar Institute of Engineering and Technology, Patiala, India.
Drug Chem Toxicol. 2024 Sep;47(5):496-506. doi: 10.1080/01480545.2023.2240542. Epub 2023 Jul 28.
The study is the first to formulate and investigate potential of papaya seed chloroform extract based solid lipid nanoparticles (PSCEN) as antifertility agents on male The prepared nanoparticles were spherical of size 300-600 nm. The release kinetics showed a controlled release of the drug with major release over 48 h. To assess the antifertility effects of PSCEN, adult male rats were fed a diet containing two different concentrations of PSCEN (5% and 10%) for 15 days under bi-choice conditions. The mean total active ingredient ingestion of the rats in the two treated groups ranged from 2.13-3.31 and 3.92-5.87 g/100g body weight, respectively. No adverse effects of treatment on body weight were observed. Also, no mortality of rats was observed. The treatment had a significant effect on the weight of the testis and the epididymis, but not on the other organs. Sperm motility (%), sperm viability (%), sperm count (millions/ml), sperm mitochondrial activity (%), sperm nuclear chromatin de-condensation (%) and sperm hypo-osmotic swelling (%) were significantly decreased, and sperm abnormality (%) significantly increased compared to the vehicle control group. The reproductive success rates of male rats treated with 5% and 10% PSCEN and mated with untreated female rats were 20.00-66.67% and 16.67%, respectively, while in untreated female rats mated with male rats of vehicle control group, reproductive success rate was 33.33 to 80%. The study found a maximal antifertility effect of the 10% PSCEN containing bait, which was irreversible up to 105 days after stopping treatment, suggesting long-term efficacy.
这项研究首次提出并研究了基于番木瓜种子氯仿提取物的固体脂质纳米粒(PSCEN)作为男性抗生育剂的潜力。所制备的纳米粒呈球形,粒径为 300-600nm。释放动力学显示药物呈控制释放,主要在 48 小时以上释放。为了评估 PSCEN 的抗生育作用,成年雄性大鼠在双选择条件下,通过饲料摄入两种不同浓度的 PSCEN(5%和 10%)15 天。两个处理组大鼠的平均总活性成分摄入量分别为 2.13-3.31 和 3.92-5.87g/100g 体重。治疗对体重没有不良影响。此外,没有大鼠死亡。该治疗对睾丸和附睾的重量有显著影响,但对其他器官没有影响。精子活力(%)、精子存活率(%)、精子计数(百万/ml)、精子线粒体活性(%)、精子核染色质去凝聚(%)和精子低渗肿胀(%)显著降低,精子畸形(%)显著增加与载体对照组相比。用 5%和 10% PSCEN 处理的雄性大鼠的生殖成功率与未经处理的雌性大鼠交配分别为 20.00-66.67%和 16.67%,而未经处理的雌性大鼠与载体对照组雄性大鼠交配,生殖成功率为 33.33%至 80%。研究发现 10% PSCEN 诱饵具有最大的抗生育作用,停止治疗后 105 天内仍具有不可逆作用,提示其具有长期疗效。