a School of Pharmacy and Medical Sciences , University of South Australia , Adelaide , South Australia , Australia.
b ARC Centre of Excellence in Convergent Bio-Nano Science and Technology , University of South Australia , Adelaide , South Australia , Australia.
Expert Opin Drug Deliv. 2019 May;16(5):507-524. doi: 10.1080/17425247.2019.1605353. Epub 2019 Apr 18.
A promising approach that has recently emerged to overcome the complex biobarriers and interrelated challenges associated with oral drug absorption is to combine the benefits of polymeric and lipid-based nanocarriers within one hybrid system. This multifaceted formulation strategy has given rise to a plethora of polymer-lipid hybrid (PLH) systems with varying nanostructures and biological activities, all of which have demonstrated the ability to improve the biopharmaceutical performance of a wide range of challenging therapeutics.
The multitude of polymers that can be combined with lipids to exert a synergistic effect for oral drug delivery have been identified, reviewed and critically evaluated. Specific focus is attributed to preclinical studies performed within the past 5 years that have elucidated the role and mechanism of the polymer phase in altering the oral absorption of encapsulated therapeutics.
The potential of PLH systems has been clearly identified; however, improved understanding of the structure-activity relationship between PLH systems and oral absorption is fundamental for translating this promising delivery approach into a clinically relevant formulation. Advancing research within this field to identify optimal polymer, lipid combinations and engineering conditions for specific therapeutics are therefore encouraged.
为了克服口服药物吸收相关的复杂生物屏障和相互关联的挑战，最近出现了一种很有前途的方法，即将聚合物和基于脂质的纳米载体的优势结合在一个混合系统中。这种多方面的配方策略产生了大量具有不同纳米结构和生物活性的聚合物-脂质混合（PLH）系统，所有这些系统都证明了能够改善多种挑战性治疗药物的生物制药性能。
已经确定、综述和批判性评估了可以与脂质结合以发挥协同作用用于口服药物递送的多种聚合物。特别关注的是过去 5 年内进行的临床前研究，这些研究阐明了聚合物相在改变包封治疗剂的口服吸收中的作用和机制。
PLH 系统的潜力已经得到明确识别；然而，为了将这种有前途的递药方法转化为临床相关制剂，深入了解 PLH 系统与口服吸收之间的结构-活性关系至关重要。因此，鼓励在该领域开展研究，以确定针对特定治疗药物的最佳聚合物、脂质组合和工程条件。
