Current approaches to paclitaxel formulation development: challenges and future perspectives (review)
Year: 2026
Type: article
Abstract: Introduction. Paclitaxel is a plant-derived antineoplastic agent with high potential in the treatment a wide range of malignant neoplasms. However, the unique properties of paclitaxel – low aqueous solubility, poor oral bioavailability, and high toxicity – create considerable challenges in the development of stable formulations, substantially limiting its clinical application. Therefore, there is an active ongoing search for novel technologies capable of enhancing the therapeutic efficacy of paclitaxel while reducing the impact of toxic effects on the human body. Text. Paclitaxel is one of the most widely used drugs for the treatment in modern oncology. Its antitumor mechanism of action is based on its ability to act on tubulin, stimulating the assembly of microtubules, stabilizing them, and thus preventing their dissociation, which leads to mitotic arrest and subsequent cell death. Paclitaxel possesses a complex structure comprising various functional groups, including ester linkages, a taxane ring, and aromatic moieties. These molecular elements determine paclitaxel's anticancer activity as well as its physicochemical properties. Paclitaxel belongs to Class IV according to the Biopharmaceutics Classification System (BCS) and has low solubility and low intestinal permeability. Drug substances of this class are the most challenging for formulation development and exhibit extremely low bioavailability. The low solubility, poor bioavailability, and high toxicity of paclitaxel pose significant challenges in pharmaceutical development. Furthermore, the polymorphism of paclitaxel can also have a significant influence on stability and biopharmaceutical properties of finished dosage forms. For example, the choice of polymorphic form can be of fundamental importance for the efficacy and safety not only of antitumor drugs but also of paclitaxel coated medical devices used in the treatment of cardiovascular diseases, in particular restenosis after angioplasty. Despite the availability of formulations successfully used in clinical practice, the development of new ones continues to this day. Nowadays, researchers face the task of enhancing paclitaxel's bioavailability while reducing its toxic effects on the human body. Conclusion. The challenges in developing paclitaxel formulations are multifaceted. New strategies for treating malignant tumors using paclitaxel are in place, and novel drug compositions and combinations are under investigation. This work reviews contemporary studies focused on the development of new dosage forms of paclitaxel.
Source: Drug development & registration
Language: English
Subfield: Pharmaceutical Science
Domain: Life Sciences
Open Access status: diamond
OpenAlex ID: W7202074958