Nanoparticles in pancreatic cancer therapy: a detailed and elaborated review on patent literature.

INTRODUCTION: Nanotechnology may open up new avenues for overcoming the challenges of pancreatic cancer therapy as a broad arsenal of anticancer medicines fail to realize their full therapeutic potential in pancreatic ductal adenocarcinoma due to the formation of multiple resistance mechanisms inside the tumor. Many studies have reported the successful use of various nano formulations in pancreatic cancer therapy. AREAS COVERED: This review covers all the major nanotechnology-based patent litrature available on renowned patent data bases like Patentscope and Espacenet, through the time period of 2007-2022. This is an entirely patent centric review, and it includes both clinical and non-clinical data available on nanotechnology-based therapeutics and diagnostic tools for pancreatic cancer. EXPERT OPINION: For the sake of understanding, the patents are categorized under various formulation-specific heads like metallic/non-metallic nanoparticles, polymeric nanoparticles, liposomes, carbon nanotubes, protein nanoparticles and liposomes. This distinguishes one specific nanoparticle type from another and makes this review a one-of-a-kind comprehensive patent compilation that has not been reported so far in the history of nanotechnological formulations in pancreatic cancer.

pH triggered delivery of curcumin from Eudragit-coated chitosan microspheres for inflammatory bowel disease: characterization and pharmacodynamic evaluation.

OBJECTIVE: This investigation deals with the development and evaluation (in vitro and in vivo) of pH triggered Eudragit-coated chitosan microspheres of curcumin (CUR) for treating ulcerative colitis. METHODS: CUR-loaded chitosan microspheres were initially prepared by emulsion cross linking method followed by coating with Eudragit S-100. The pharmacodynamics of the developed formulation was analyzed in mice by acetic acid induced colitis model. RESULTS: The developed microspheres were of uniform spherical shape with high entrapment efficiency. CUR-chitosan microspheres showed less intense peaks compared to free CUR confirming inclusion of drug within microspheres as revealed by X-ray diffractogram. Uncoated CUR-chitosan microspheres exhibited burst release within initial 4 h while microspheres coated with Eudragit S-100 prevented premature release of CUR and showed controlled release up to 12 h following Higuchi model. In vivo organ biodistribution study showed negligible amount of CUR in stomach and small intestine confirming integrity of microsphere in upper gastrointestinal tract (GIT). In vivo study revealed significant reduction in severity and extent of colonic damage with CUR-loaded microspheres as compared to pure CUR which was further confirmed by histopathological study. CONCLUSION: In vitro and in vivo studies proved the developed formulations as a promising system for pH-dependent delivery of drug to colon in ulcerative colitis.

Garden rue inhibits the arachidonic acid pathway, scavenges free radicals, and elevates FRAP: role in inflammation.

AIM: In the present study, the anti-inflammatory and antioxidant activities of the methanol extract of Ruta graveolens leaves (RG-M) were evaluated using various in vivo and in vitro models. METHOD: For anti-inflammatory activity, RG-M was administered by the oral route (p.o.) in a carrageenan-induced paw edema model, and by the intraperitoneal route (i.p.) in an exudative inflammation model. In vitro inhibition of cyclooxygenase and lipoxygenase enzymes was evaluated. In vitro antioxidant activity was also examined. Endogenous antioxidant status was further evaluated by ferric reducing ability of plasma model. RESULTS: RG-M showed maximum inhibition of carrageenan-induced edema (100 mg·kg⁻¹ - 33.36%; 200 mg·kg⁻¹ - 45.32% and 400 mg·kg⁻¹ - 56.28%). In the exudative inflammation model, a significant reduction in leukocyte migration (200 mg·kg⁻¹ - 54.75% and 400 mg·kg⁻¹ - 77.97%) and protein exudation (200 mg·kg⁻¹ - 31.14% and 400 mg·kg⁻¹ - 49.91%) were observed. RG-M also exhibited inhibition of COX-1 (IC50 182.27 µg·mL⁻¹) and COX-2 (IC50 190.16 µg·mL⁻¹) as well as 5-LOX (IC50 215.71 µg·mL⁻¹). Antioxidant activity was significant with improved endogenous antioxidant status. CONCLUSION: The results demonstrated the anti-inflammatory and antioxidant activity of RG-M with potent inhibitory effects on the arachidonic acid pathways.