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抗癫痫药物递送的潜在新方法。

Potential new methods for antiepileptic drug delivery.

作者信息

Fisher Robert S, Ho Jet

机构信息

Stanford Comprehensive Epilepsy Center, Stanford University Medical Center, Stanford, California 94305-5235, USA.

出版信息

CNS Drugs. 2002;16(9):579-93. doi: 10.2165/00023210-200216090-00001.

Abstract

Use of novel drug delivery methods could enhance the efficacy and reduce the toxicity of antiepileptic drugs (AEDs). Slow-release oral forms of medication or depot drugs such as skin patches might improve compliance and therefore seizure control. In emergency situations, administration via rectal, nasal or buccal mucosa can deliver the drug more quickly than can oral administration. Slow-release oral forms and rectal forms of AEDs are already approved for use, nasal and buccal administration is currently off-label and skin patches for AEDs are an attractive but currently hypothetical option. Therapies under development may result in the delivery of AEDs directly to the regions of the brain involved in seizures. Experimental protocols are underway to allow continuous infusion of potent excitatory amino acid antagonists into the CSF. In experiments with animal models of epilepsy, AEDs have been delivered successfully to seizure foci in the brain by programmed infusion pumps, acting in response to computerised EEG seizure detection. Inactive prodrugs can be given systemically and activated at the site of the seizure focus by locally released compounds. One such drug under development is DP-VPA (or DP16), which is cleaved to valproic acid (sodium valproate) by phospholipases at the seizure focus. Liposomes and nanoparticles are engineered micro-reservoirs of a drug, with attached antibodies or receptor-specific binding agents designed to target the particles to a specific region of the body. Liposomes in theory could deliver a high concentration of an AED to a seizure focus. Penetration of the blood-brain barrier can be accomplished by linking large particles to iron transferrin or biological toxins that can cross the barrier. In the near future, it is likely that cell transplants that generate neurotransmitters and neuromodulators will accomplish renewable endogenous drug delivery. However, the survival and viability of transplanted cells have yet to be demonstrated in the clinical setting. Gene therapy also may play a role in local drug delivery with the use of adenovirus, adeno-associated virus, herpesvirus or other delivery vectors to induce brain cells to produce local modulatory substances. New delivery systems should significantly improve the therapeutic/toxic ratio of AEDs.

摘要

使用新型药物递送方法可提高抗癫痫药物(AEDs)的疗效并降低其毒性。缓释口服剂型或长效药物(如皮肤贴片)可能会提高依从性,从而更好地控制癫痫发作。在紧急情况下,通过直肠、鼻腔或口腔黏膜给药比口服给药能更快地递送药物。AEDs的缓释口服剂型和直肠剂型已获批使用,鼻腔和口腔给药目前属于超说明书用药,而AEDs皮肤贴片是一个有吸引力但目前只是设想中的选择。正在研发的疗法可能会使AEDs直接递送至大脑中与癫痫发作相关的区域。正在进行实验方案,以允许将强效兴奋性氨基酸拮抗剂持续输注到脑脊液中。在癫痫动物模型实验中,通过编程输液泵成功地将AEDs递送至大脑中的癫痫病灶,该输液泵根据计算机化脑电图癫痫检测进行响应。无活性前体药物可全身给药,并在癫痫病灶部位被局部释放的化合物激活。一种正在研发的此类药物是DP - VPA(或DP16),它在癫痫病灶处被磷脂酶裂解为丙戊酸(丙戊酸钠)。脂质体和纳米颗粒是经过工程设计的药物微储库,带有附着的抗体或受体特异性结合剂,旨在将颗粒靶向至身体的特定区域。理论上,脂质体可将高浓度的AED递送至癫痫病灶。通过将大颗粒与可穿过血脑屏障的转铁蛋白或生物毒素相连,可实现血脑屏障的穿透。在不久的将来,产生神经递质和神经调节剂的细胞移植可能会实现可再生的内源性药物递送。然而,移植细胞在临床环境中的存活和活力尚未得到证实。基因治疗也可能在局部药物递送中发挥作用,使用腺病毒、腺相关病毒、疱疹病毒或其他递送载体来诱导脑细胞产生局部调节物质。新的递送系统应能显著提高AEDs的治疗/毒性比。

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