Umbelliprenin-loaded nanostructured lipid carrier: A novel approach for inducing cytotoxicity and apoptosis in colorectal cancer cells by altering the p53, survivin, and Bax/Bcl2 ratio

Introduction: Conduction of cancer cells towards apoptosis is the main approach in cancer therapy. Umbelliprenin (Umb), the naturally occurring agent, induces apoptosis in often cancerous cells. Employing nanostructured lipid carriers (NLCs) to encapsulate Umb for boosting apoptosis in colorectal cancer cells was the main goal of this study. Methods: The hot homogenizer manner produced Umb loading NLCs were examined in terms of particle size, zeta potential, morphology, encapsulation efficiency (EE), in vitro release, and cytotoxicity. Annexin/PI and DAPI staining tests were performed to indicate apoptosis in HT-29 cells treated with NLC/Umb. Additionally, RT-PCR was done to evaluate the expression of some apoptosis-related genes. Results: Resulting data demonstrated a size of 145.1 +/- 94.65 nm, 0.277 PDI value, and zeta potential of 4.99 +/- 5.16 mv. Moreover, high EE was observed (up to 85 %). The in vitro release study proved a Umb biphasic release pattern. Besides, the result displayed that the HT-29 cell uptakes of NLC/Umb happened in a time-dependent manner. NLC containing Umb nano-formulation exhibited significantly higher cytotoxicity (p < 0.05) and apoptosis (p < 0.001) in comparison with the control group, blank NLC, and free Umb. Based on real-time PCR outcome, significant (p < 0.05) upregulation in P53 and Bax and a notable downregulation in survivin and Bcl-2 were revealed in HT-29 cells incubating with NLC/Umb than in the control group. Conclusion: The obtained data recommended that Umb-loaded NLC can be a reliable and effective treatment against colorectal cancer cells that exert its impact through impressing apoptosis associated with key genes.

Automated summary

This study aimed to enhance apoptosis in colorectal cancer cells by encapsulating Umbelliprenin (Umb) in nanostructured lipid carriers (NLCs). The results demonstrated that Umb-loaded NLCs had favorable particle size, encapsulation efficiency, and release pattern, and showed significantly increased cytotoxicity and apoptosis in tumor cells by upregulating P53 and Bax and downregulating survivin and Bcl-2.