Curcumin, a functional food polyphenol reported to inhibit cancer cell proliferation, invasion, angiogenesis and metastasis through interaction with multiple molecular targets. However, the clinical usefulness of curcumin in the treatment of cancer is limited due to poor solubility in water at acidic and neutral pH, hydrolytic degradation in alkaline pH and metabolism in the liver and intestine, resulting in decreased or absence of therapeutic efficacy. Hence, the present study was aimed to overcome the limitations of curcumin in the treatment of cancer by codelivery of nanosized curcumin and bioenhancer using acid degradable polymeric nanoparticles. Modified nanoprecipitation method was used to prepare void, curcumin-piperine, curcumin-quercetin and curcumin-silibinin encapsulated polymeric nanoparticles. Prepared nanoformulations were evaluated for particle size, polydispersity index, zeta potential, surface morphology, drug content, encapsulation efficiency, drug loading, invitro release, stability at elevated storage conditions, toxicity on normal liver cells, anticancer activity on various cancer cell lines and on cancer induced rats. Prepared curcumin-bioenhancer encapsulated polymeric nanoparticles were (a) spherical in shape with size <100 nm and displayed excellent uniformity; (b) showed >95% release of curcumin and bioenhancers within 45 minutes in gastric fluid; (c) proved non-toxic to normal liver cells; (d) extremely stable at elevated storage conditions; and (e) demonstrated enhanced anticancer activity against various cancer cell lines and mammary cancer in rats than the pure curcumin. Study concludes that the prepared curcumin-bioenhancer encapsulated polymeric nanoformulations significantly overcome the limitations of curcumin in the treatment of cancer and synergistically enhance its anticancer activity. However, out of three polymeric nanoformulations, curcumin-silibinin polymeric nanoformulation showed superior anticancer activity.
The present study was aimed to develop dimethylaminoethyl methacrylate based nanoparticulate drug delivery system using nanoprecipitation method and optimize the process parameters using PlackettBurman factorial design to yield least average particle size and narrow sized particle distribution without filtration or centrifugation process. Twelve experimental runs involving 11 process parameters at higher and lower levels were generated using Design-Expert. Factorial design result has shown that (a) Except stirring duration all other process parameters significantly influence the average particle size; (B) Except β-cyclodextrin concentration, aqueous phase volume and organic phase volume, all other process parameters significantly influence the polydispersity index; and (C) Except polymer concentration and poloxamer 407 concentration, all other process parameters do not significantly influence the zeta potential. The average particle size, polydispersity index and zeta potential of the prepared dual drug loaded nanoparticles were well within acceptable limits and found to be in the range of 47 to 87 nm, 0.14 to 0.28 and 22 to 39 mV, respectively. Surface morphology examination has shown that the prepared nanoparticles were spherical in shape. The developed dimethylaminoethyl methacrylate based nanoparticulate drug delivery system can be routinely used to fabricate narrow sized polymeric nanoparticles without filtration or centrifugation process.
The present study was aimed to fabricate Curcumin loaded Eudragit E 100 polymeric nanoparticles and to study the effect of various manufacturing parameters on the average particle size, span, uniformity and surface area of the prepared polymeric nanoparticles by utilizing Plackett-Burman experimental designs. Curcumin loaded Eudragit E 100 nanoparticles were prepared by nanoprecipitation method and characterized using particle size analyser. Plackett-Burman design was implemented to study the influence of eight independent variables on three dependent variables. Twelve experimental trials involving 8 independent variables at higher and lower levels were generated by Design-Expert. Out of 12 trials, 4 th and 9 th trails were within the acceptable limits. Least average particle size can be obtained by increasing the concentration of poloxamer 188, increasing the volume of aqueous phase, increasing the sonication duration and decreasing the ethanol concentration. Similarly, span less than 1 can be obtained by increasing the concentration of poloxamer 188, increasing the sonication duration and decreasing the ethanol concentration. However, uniformity can be increased decreasing the ethanol concentration. Higher surface area can be obtained by increasing the concentration of Eudragit E 100, poloxamer 188 and increasing the volume of the aqueous phase.
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