Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2023 Feb 1;15(2):484.
doi: 10.3390/pharmaceutics15020484.

Advances in Oral Drug Delivery Systems: Challenges and Opportunities

Jie Lou  1   2 , Hongli Duan  1 , Qin Qin  1 , Zhipeng Teng  3 , Fengxu Gan  1 , Xiaofang Zhou  1 , Xing Zhou  1   2   4
Affiliations
Review

Advances in Oral Drug Delivery Systems: Challenges and Opportunities

Jie Lou et al. Pharmaceutics. .

Abstract

The oral route is the most preferred route for systemic and local drug delivery. However, the oral drug delivery system faces the harsh physiological and physicochemical environment of the gastrointestinal tract, which limits the bioavailability and targeted design of oral drug delivery system. Innovative pharmaceutical approaches including nanoparticulate formulations, biomimetic drug formulations, and microfabricated devices have been explored to optimize drug targeting and bioavailability. In this review, the anatomical factors, biochemical factors, and physiology factors that influence delivering drug via oral route are discussed and recent advance in conventional and novel oral drug delivery approaches for improving drug bioavailability and targeting ability are highlighted. We also address the challenges and opportunities of oral drug delivery systems in future.

Keywords: gastrointestinal barriers; novel drug delivery system; oral drug delivery system; oral nanomedicine; oral target delivery.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Local targeting drug delivery systems to GIT after oral administration.
Figure 2
Figure 2
Targeting delivery systems to non-gastrointestinal diseases after oral administration.
Figure 3
Figure 3
Schematic diagram of YC-mediated nanoparticles to inflammation-associated diseases [118]. Reproduced from ref. [118] with permission from the American Chemical Society, copyright 2017.
Figure 4
Figure 4
Schematic diagram of a CDDP nanoprecursor for targeted tumor treatment [120]. Reproduced from ref. [120] with permission from the author.
Figure 5
Figure 5
Schematic illustration of the fabrication and transepithelial transport mechanism of DOX/SOR/Spore-DA [121]. Reproduced from ref. [121] with permission from the John Wiley and Sons, copyright 2018.
Figure 6
Figure 6
Schematic diagram of LAM-mediated oral targeting of nanoparticles to multiple sites of obesity related diseases [122]. Reproduced from ref. [122] with permission from the author.
Figure 7
Figure 7
Schematic diagram of the noninvasive gut-to-brain oral drug delivery system [124]. Reproduced from ref. [124] with permission from John Wiley and Sons, copyright 2021.
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. He S., Liu Z., Xu D. Advance in oral delivery systems for therapeutic protein. J. Drug Target. 2019;27:283–291. doi: 10.1080/1061186X.2018.1486406. - DOI - PubMed
    1. Hua S. Advances in oral drug delivery for regional targeting in the gastrointestinal tract—Influence of physiological, pathophysiological and pharmaceutical factors. Front. Pharmacol. 2020;11:524. doi: 10.3389/fphar.2020.00524. - DOI - PMC - PubMed
    1. Majumder J., Taratula O., Minko T. Nanocarrier-based systems for targeted and site specific therapeutic delivery. Adv. Drug Deliv. Rev. 2019;144:57–77. doi: 10.1016/j.addr.2019.07.010. - DOI - PMC - PubMed
    1. Reinholz J., Landfester K., Mailander V. The challenges of oral drug delivery via nanocarriers. Drug Deliv. 2018;25:1694–1705. doi: 10.1080/10717544.2018.1501119. - DOI - PMC - PubMed
    1. Shan W., Zhu X., Liu M., Li L., Zhong J., Sun W., Zhang Z., Huang Y. Overcoming the diffusion barrier of mucus and absorption barrier of epithelium by self-assembled nanoparticles for oral delivery of insulin. ACS Nano. 2015;9:2345–2356. doi: 10.1021/acsnano.5b00028. - DOI - PubMed

LinkOut - more resources