Huang Zhengwei, Shu Lei, Huang Ying, Wu Chuanbin, Pan Xin
College of Pharmacy, Jinan University, Guangzhou 510632, China.
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Pharmaceuticals (Basel). 2022 Mar 23;15(4):389. doi: 10.3390/ph15040389.
Peptide-based drugs have attracted extensive attention from the medical and pharmaceutical industry because of their relatively high safety and efficacy. However, most of the peptide drugs approved are administrated by injection, which can easily cause poor patient compliance. In this circumstance, pulmonary administration as an alternative to injection administration can not only avoid the above issue but also accelerate the absorption rate of peptide drugs and improve bioavailability. Among the pulmonary delivery systems available on the market, metered-dose inhalers (MDIs) have emerged as appealing candidates for pulmonary delivery systems with clinical translational value, owing to their many merits, including portable, easy-to-operate, and cost-effective properties. Nevertheless, the industrialization of peptide drugs-containing MDIs encounters a bottleneck of low drug loading, owing to the incompatibility between the propellant and the peptide drugs, which cannot be effectively overcome by the current carrier particle encapsulation strategy. Herein, we put forward the following strategies: (1) To screen amphiphilic materials with high surface activity and strong interaction with peptide drugs; (2) To construct a chemical connection between peptide drugs and amphiphilic substances; (3) To optimize the cosolvent for dispersing peptide drugs. We suppose these strategies have the potential to defeat the bottleneck problem and provide a new idea for the industrialization of peptide drugs-containing MDIs.
基于肽的药物因其相对较高的安全性和有效性而受到医药行业的广泛关注。然而，大多数已获批的肽类药物通过注射给药，这很容易导致患者依从性差。在这种情况下，肺部给药作为注射给药的替代方式，不仅可以避免上述问题，还能加快肽类药物的吸收速度并提高生物利用度。在市场上现有的肺部给药系统中，定量吸入器（MDIs）因其诸多优点，包括便携、易于操作和成本效益高，已成为具有临床转化价值的肺部给药系统的有吸引力的候选者。然而，由于推进剂与肽类药物之间的不相容性，含肽药物的MDIs的产业化遇到了药物负载量低的瓶颈，而目前的载体颗粒包封策略无法有效克服这一问题。在此，我们提出以下策略：（1）筛选具有高表面活性且与肽类药物有强相互作用的两亲性材料；（2）在肽类药物与两亲性物质之间构建化学连接；（3）优化用于分散肽类药物的助溶剂。我们认为这些策略有可能克服瓶颈问题，并为含肽药物的MDIs的产业化提供新思路。
