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ABSTRACTThe release of active agents in tumors rather than normal tissues, limits systemic exposure and toxicities. Targeting over-expressed esterase enzyme in the tumor microenvironment can selectively release immune-active agents like Programmed Death-1 (PD-1) and PD-1 ligand inhibitors from ester-sensitive lipid nanocarriers, offering a novel approach compared with conventional therapies. PD-1 and PD-L1 association cause T-cell inactivation, whereas blocking their association improves their cytotoxic mechanism. The patent application US2022/0080051-A1 discloses a novel immune-active agent conjugated with lipid to form a nanocarrier for esterase-sensitive release. These nanocarriers selectively enter leaky vasculature of tumors through enhanced permeability and retention effect, undergo ester cleavage to release agents, and are reported to increase bioavailability by 24 times. Further, with other agents or alone it achieves targeted synergistic cancer therapy. Also, the current patent spotlight delves into the crucial formulation considerations necessary for obtaining successful approval of lipidic nano products from relevant regulatory authorities.

Pancreatic adenocarcinoma, a devastating disease, has the worst cancer prognosis in humans. It often develops resistance to common chemotherapy medications, such as gemcitabine, taxol and 5-fluorouracil. The dense stroma limits therapeutic efficacy in treating this disease. Low or limited drug loading capacity is another problem with current chemotherapeutic agents. There is a need to develop novel approaches to overcome these issues. Hence, an innovative approach has been proposed to co-deliver both hydrophilic (Gemcitabine) and hydrophobic (Paclitaxel) drugs in a single carrier using lipid bilayer-mesoporous silica nanoparticles (LB-MSNP). MSNPs offer effective drug delivery due to their superior bioavailability and physicochemical properties. Further, in order to achieve clinical translation and regulatory approval, toxicity and biodegradability of MSNPs must be resolved.

Pancreatic adenocarcinoma, a devastating disease, has the worst cancer prognosis in humans. It often develops resistance to common chemotherapy medications, such as gemcitabine, taxol and 5-fluorouracil. The dense stroma limits therapeutic efficacy in treating this disease. Low or limited drug loading capacity is another problem with current chemotherapeutic agents. There is a need to develop novel approaches to overcome these issues. Hence, an innovative approach has been proposed to co-deliver both hydrophilic (Gemcitabine) and hydrophobic (Paclitaxel) drugs in a single carrier using lipid bilayer-mesoporous silica nanoparticles (LB-MSNP). MSNPs offer effective drug delivery due to their superior bioavailability and physicochemical properties. Further, in order to achieve clinical translation and regulatory approval, toxicity and biodegradability of MSNPs must be resolved.

Photoresponsive liposome development is needed to serve as a facile alternative to ELISA which is ineffective for detecting small levels of biomarkers due to low detection sensitivity. The US20210396744 patent application outlines novel photoresponsive liposomes for the detection of target substances with the aid of light. Although versatile, there may be possible stability issues that can be avoided with the appropriate selection of liposome components. Furthermore, the clinical success of this technology depends on many parameters like plasma stability, efficient loading of photosensitive components in the membrane and immobilization of molecular recognition elements to the membrane. Despite several challenges, they possess enormous potential to become a non-invasive tool for the detection of target substances.

Aim:To overcome the limitations associated with conventional formulations for cancer treatment by the effective utilization of nanoemulsion with therapy and diagnosis through the single unit. Patent:US20210275687 describes the usage of functionalized various oil-in-water nanoemulsions as pharmacological vehicles with theranostic potential in cancer treatment. Materials & methods:Vitamin E, oleic acid, sphingomyelin, ligands for functionalization, contrast agents and therapeutic biomolecules. Results:The toxicity studies conducted on healthy mice did not show any apparent toxicity issues. The stability studies conducted at 40 °C and 75% relative humidity, which is mandatory for regulatory approval, indicated the adequate physical stability of the formulation. Conclusion:The studies exhibited the promising theranostic potential of the developed nanoemulsion for the effective management and diagnosis of cancer and metastatic diseases.