Statistically developed stable Camptothecin-loaded Soluplus/TPGS mixed micelles for improved ovarian cancer treatment

In this research, Camptothecin-loaded mixed micelles (CPT-MMs) were formulated by combining Soluplus®, a novel amphiphilic excipient, with D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS). The use of appropriate excipients is crucial in stabilizing micellar structures and improving drug entrapment efficiency. TPGS, with its ability to self-assemble into micelles, was an ideal candidate, and incorporating Soluplus further enhanced micelle stability and drug-loading capacity. A 32 full factorial design was employed to investigate the influence of key factors on particle size and %entrapment efficiency (%EE).

The statistical analysis using Design Expert® VR software provided meaningful conclusions on the significance of each factor and their interactions, facilitating the successful optimization of CPT-MMs dispersion with improved drug delivery capabilities. The mean particle size, zeta potential, %drug loading capacity (%DLC), and (%EE) of CPT-MMs were 77.8 ± 2.67 nm, −23.4 ± 0.36 mV, 45.6 ± 1.78%, and 68.61 ± 1.8% respectively. CPT-MMs demonstrated sustained-release characteristics, preventing premature drug release and enhancing drug accumulation in tumor tissues, potentially optimizing CPT delivery for cancer treatment. Importantly, CPT-MMs dispersion exhibited lower hemolysis compared to plain CPT, indicating excellent biocompatibility and safety for intravenous administration.

The sustained release of CPT from CPT-MMs dispersion may lead to reduced cytotoxicity and improved therapeutic efficacy. Additionally, the lyophilized formulation showed superior stability compared to the liquid micelles. In conclusion, the development of CPT-MMs presents a promising strategy for enhancing drug delivery and optimizing therapeutic outcomes in cancer treatment. The sustained-release feature, along with enhanced biocompatibility and stability, holds great potential for the clinical translation of these MMs as efficient drug delivery systems for ovarian cancer treatment.

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Shruti Kargane, Rutuja Chougale, Nitin Mali, Kiran Patil, Shalaka Patki & John Disouza, Statistically developed stable Camptothecin-loaded Soluplus/TPGS mixed micelles for improved ovarian cancer treatment, Received 08 Aug 2023, Accepted 08 Jan 2024, Published online: 12 Feb 2024, https://doi.org/10.1080/01932691.2024.2304634

Read more on TPGS here and watch also the interesting video on Vitamin E TPGS: