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首页> 外文期刊>International Journal of Pharmaceutics >Oral delivery of oil-based formulation for a novel synthetic cationic peptide of GnRH (gonadotropin-releasing hormone) antagonist for prostate cancer treatment
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Oral delivery of oil-based formulation for a novel synthetic cationic peptide of GnRH (gonadotropin-releasing hormone) antagonist for prostate cancer treatment

机译：口服合成新型GnRH（促性腺激素释放激素）拮抗剂的阳离子肽的油基制剂，用于前列腺癌的治疗

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摘要

LXT-101, a cationic peptide is a novel antagonist of gonadotropin-releasing hormone (GnRH) for prostate cancer treatment. However, effective delivery of peptide drugs into the body by the oral route remains a major challenge due to their origin properties with high molecular weights, strong polarity and low stability in the gastrointestinal (GI) tract. In this study, we have developed a novel oral delivery of oil-based formulation in which therapeutic peptide LXT-101 are solubilized in oils and with this solution as oil phase, an optimum formulation of self-microemulsifying drug delivery system (SMEDDS) was developed. The peptide stability with the SMEDDS formulation in artificial gastric and intestinal fluid was tested in vitro. On the other hand, the testosterone level and plasma concentration of LXT-101 in rats after oral administration of the SMEDDS formulation were investigated in vivo. The data in vitro indicated that LXT-101 in the SMEDDS formulation was stable over 8 h in artificial gastric and intestinal fluid. LXT-101 can be absorbed in vivo and suppression of testosterone maintained in castration level within 12 h can be achieved effectively after SMEDDS formulation administered orally at a dose of 3.5 mg/kg. The approach can provide a potential way for delivery peptides by oral.
机译：阳离子肽LXT-101是促性腺激素释放激素（GnRH）的新型拮抗剂，可治疗前列腺癌。然而，由于其高分子量，强极性和胃肠道（GI）稳定性的起源特性，通过口服途径将肽药物有效地递送入体内仍然是主要的挑战。在这项研究中，我们开发了一种新的口服油基制剂，其中将治疗性肽LXT-101溶于油中，并以该溶液为油相，开发了一种自微乳化药物输送系统（SMEDDS）的最佳制剂。 。用SMEDDS制剂在人工胃液和肠液中的肽稳定性进行了体外测试。另一方面，在体内研究了口服SMEDDS制剂后大鼠的睾丸激素水平和LXT-101的血浆浓度。体外数据表明，SMEDDS制剂中的LXT-101在人造胃液和肠液中稳定超过8小时。 LXT-101可以在体内吸收，在以3.5 mg / kg的剂量口服SMEDDS制剂后，可以在12小时内有效地抑制睾丸激素维持在去势水平。该方法可以提供通过口服递送肽的潜在途径。

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