Posted by Phytosomes represent an innovative approach to herbal medicine delivery that has garnered considerable attention in recent years. These novel formulations involve the complexation of phytoconstituents with phospholipids to enhance their bioavailability and therapeutic efficacy. By forming stable complexes with phospholipids, phytosomes overcome the limitations of poor solubility and absorption often associated with herbal extracts, thereby facilitating improved delivery and cellular uptake of bioactive compounds. This unique lipid-based delivery system enhances the pharmacokinetic properties of herbal extracts and allows for targeted delivery to specific tissues or cells of interest. As a result, phytosomes have emerged as promising vehicles for delivering herbal medicines, offering the potential to optimize their therapeutic benefits in various clinical applications, including cancer treatment.
In this work (1) formulation preparation was conducted using the thin film hydration technique: the known weight of the drug (in this case hinokitiol) (100 mg) and the calculated amount of phospholipid, cholesterol, and sodium deoxycholate were dissolved in ethanol with the aid of water bath sonication . Subsequently, the organic solvent (ethanol) was evaporated at 45°C under reduced pressure until a thin lipid film was formed inside the container. Then, a known volume of the specified water was added to the lipid film, and the mixture was stirred at 50°C for 30 minutes. Finally, the mixture was subjected to high-speed homogenization at 20,000 rpm for 10 minutes to achieve uniform dispersion.
The optimized phytosomes demonstrated a size range of 138.4 ± 7.7 to 763.7 ± 15.4 nm, with zeta potentials ranging from − 10.2 ± 0.28 to − 53.2 ± 1.06 mV and entrapment efficiencies between 29.161 ± 1.163% and 92.77 ± 7.01%. Morphological characterization confirmed uniformity and spherical morphology. Hinokitiol solubility increased with pH, and the release from the optimized phytosomes exhibited sustained patterns. The formulated phytosomes showed superior cytotoxicity, with lower IC50 values compared to pure hinokitiol. Treatment induced significant apoptosis and cell cycle arrest at the G2/M and S phases.
The CD-based hinokitiol formulations were studied by the teams of profs Furuta and Kanamoto (2, 3). Calculation of the MIC value of HT using the agar dilution method revealed that the MIC of HT/CD inclusion complexes was lower than that of HT alone. HT irreversibly inhibited the growth of microorganisms in a short amount of time. HT/CD complexes retained the antimicrobial activity of HT as a result of including HT in a CD complex (3). These results suggest that inclusion of HT, an antimicrobial component, using CDs could lead to appropriate control of the drug release rate and efficient display of antimicrobial activity.
Ahmed TA, Milibary GA, Almehmady AM, Alahmadi AA, Ali EMM, El-Say KM: Improving the Cytotoxic Activity of Hinokitiol from Drug-Loaded Phytosomal Formulation Against Breast Cancer Cell Lines. Int J Nanomedicine. 2024;19:10321-10339. https://doi.org/10.2147/IJN.S476667
Furuta, T., Kusuya, Y., Neoh, Tl. et al. Inclusion and Release of Hinokitiol into/from MCT-β-CD Fixed on Japanese Washi Paper. J Incl Phenom Macrocycl Chem 56, 107–111 (2006). https://doi.org/10.1007/s10847-006-9070-9
Yutaka Inoue, Rina SuzukiIsamu, MurataHarue Nomura, Yasunori IsshikiIkuo, Kanamoto: Evaluation of Antibacterial Activity Expression of the Hinokitiol/Cyclodextrin Complex Against Bacteria. ACS Omega 2020, 5, 42, 27180–27187. https://doi.org/10.1021/acsomega.0c03222
Featured scheme: Charana Sriya K, Sai D, Ravi Sankar P. Phytosomes : A Novel Approach for Herbal Phytochemicals for Enhancing the Bioavailability N Review. Int J Pharm Sci Rev Res. 2020;60:21–26.)