CNRS, University of Bordeaux, Bordeaux, France.
Pharm Dev Technol. 2020 Feb;25(2):133-148. doi: 10.1080/10837450.2019.1689402. Epub 2019 Nov 24.
Most of biopharmaceuticals in clinical use today are available in a solution or suspension form and delivered by invasive routes (i.e. injection). However, several attempts have been made in order to develop effective oral formulations of 'biomolecules' characterized by a fragile structure and a low bioavailability. To achieve an efficient delivery of such molecules by non-parenteral route, in particular, the oral route, novel concepts are needed not only to overcome significant enzymatic and diffusion barriers but also to ensure stability and biological activity. Vaccines and antibodies have a special interest as biomolecules because of their high therapeutic efficacy both in prevention and treatment of several chronic diseases. In this review, we would like to highlight the trends made in the development of pharmaceutical forms to deliver these molecules by the oral route. Hence, we will focus on the description of the different forms (solutions, suspensions, powders, tablets, micro and nanocarriers …) available today or under research study, in which product stability and efficacy are maintained. A special attention will be paid to the formulation strategies that may include the addition of several functional excipients and/or adjuvants, aiming to protect, to functionalize or to modulate their release in the body.
今天临床上使用的大多数生物制药都是以溶液或悬浮液的形式存在，并通过侵入性途径（即注射）给药。然而，人们已经尝试了几种方法来开发具有脆弱结构和低生物利用度的“生物分子”的有效口服制剂。为了通过非肠道途径（特别是口服途径）实现此类分子的有效递药，不仅需要新的概念来克服显著的酶和扩散屏障，还需要确保稳定性和生物活性。疫苗和抗体因其在预防和治疗多种慢性疾病方面的高治疗效果，作为生物分子具有特殊的意义。在这篇综述中，我们希望强调开发用于通过口服途径递送这些分子的药物制剂形式的趋势。因此，我们将重点描述今天可用或正在研究的不同形式（溶液、悬浮液、粉末、片剂、微载体和纳米载体等），其中产品稳定性和功效得以保持。特别关注可能包括添加几种功能赋形剂和/或佐剂的制剂策略，旨在保护、功能化或调节它们在体内的释放。
