Asenapine maleate (ASPM) is an antipsychotic drug prescribed for the treatment of schizophrenia and bipolar disorder. ASPM possesses low oral bioavailability due to extensive hepatic metabolism. Therefore, RGD peptide conjugated liposomes loaded with ASPM were prepared to target Peyer's patches in the intestine which in-turn get access into intestinal lymphatic system thereby increasing the oral bioavailability of the drug. Liposomes were evaluated for size, zeta potential, differential scanning calorimetry (DSC), FTIR spectroscopy, X-ray diffraction (XRD), shape and morphology, in vitro drug release, cell line studies, everted intestinal uptake, pharmacodynamics, pharmacokinetics, tissue distribution, targetability and stability studies. In vitro drug release study showed the sustained release of drug from the formulations. Optimized liposomes (size <110 nm) showed greater permeability across the Caco2 + Raji B co-culture model in vitro and everted rat ileum ex vivo. Liposomes showed increase in bioavailability and high efficacy in reducing the L-DOPA-carbidopa induced locomotor count compared to plain drug. Liposomes also showed high concentration of drug in the brain after their oral administration. Imaging studies showed that RGD peptide conjugated liposomes were successful in targeting the Peyer's patches, both in vivo and ex vivo. The study successfully demonstrated the improved pharmacokinetics and efficacy profile of ASPM by using a ligand conjugated targeted liposomal system.

阿塞那平马来酸盐 (ASPM) 是一种抗精神病药物，用于治疗精神分裂症和双相情感障碍。由于广泛的肝脏代谢，ASPM 具有低的口服生物利用度。因此，制备了装载有 ASPM 的 RGD 肽偶联脂质体，以靶向肠道中的 Peyer 斑块，从而进入肠道淋巴系统，从而提高药物的口服生物利用度。评估脂质体的大小、zeta 电位、差示扫描量热法 (DSC)、FTIR 光谱、X 射线衍射 (XRD)、形状和形态、体外药物释放、细胞系研究、外翻肠吸收、药效学、药代动力学、组织分布，靶向性和稳定性研究。体外药物释放研究显示药物从制剂中持续释放。优化的脂质体（大小<110纳米）表明跨越的Caco2 +的Raji乙共培养模型更好的透气性在体外和外翻的大鼠回肠体外。与普通药物相比，脂质体在减少 L-DOPA-卡比多巴诱导的运动计数方面表现出更高的生物利用度和高效能。口服给药后，脂质体在大脑中也显示出高浓度的药物。影像学研究表明，RGD 肽偶联脂质体在体内和体外均成功靶向 Peyer 集结. 该研究成功证明了通过使用配体偶联的靶向脂质体系统改善了 ASPM 的药代动力学和功效特征。