Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

Khatik, Renuka; Dwivedi, Pankaj; Shukla, Ankita; Srivastava, Pallavi; Rath, Srikanta Kumar; Paliwal, Sarvesh; Dwivedi, Anil Kumar

doi:10.3109/10717544.2014.936988

Cited by 30 publications

(17 citation statements)

References 36 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The urgent need of developing more effective formulation strategies for the improved outcome of CUR resulted in evolution of several drug delivery systems (DDS) [11][12][13]. Enhanced potency of CUR by a number of alternative DDS have been investigated, which includes liposomes, polymerbased micro/nanoparticles and polymeric micelles [14][15][16][17][18].…”

Section: Introductionmentioning

confidence: 99%

Core–shell microencapsulation of curcumin in PLGA microparticles: programmed for application in ovarian cancer therapy

Dwivedi

Yuan

Han

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

Self Cite

View full text Add to dashboard Cite

In our study, we have established a novel liquid-driven co-flow focusing (LDCF) process to fabricate curcumin (CUR)-loaded poly (lactic-co-glycolic acid) (PLGA) microparticles (CPMs). LDCF-CPMs of size 20.26 ± 2.37 lm have high encapsulation efficiency (>70%) and were intended for application in ovarian cancer by intraperitoneal (IP) administration. LDCF-CPMs have smooth surface with narrow size distribution and a core-shell structured verified by confocal microscopy which can be precisely controlled by changing the flow rates of focusing, outer and inner phases. The LDCF-CPMs reveal the physiochemical stability with sustained release profile corresponding to 95% CUR release over a period of 14 days in an in vitro release medium. Moreover, LDCF-CPMs were testified for cytotoxicity against SKOV-3 ovarian cancer cell lines and peritoneal delivery advantages by animal experiments. The pharmacokinetics of LDCF-CPMs in rats following IP injection shows slow systemic absorption with mean residence time (MRT) of 13.54 h in comparison with 9.82 and 6.74 h for SE-CPMs and free CUR, respectively. In addition, IP delivery of CUR can expose the ovarian tumour to higher concentration for a longer duration by programming the thickness of the shell. The study provides compelling evidence for LDCF-CPMs having high therapeutic opportunity in the treatment of peritoneal cancers, such as ovarian, that reside in the peritoneal cavity.

show abstract

Section: Introductionmentioning

confidence: 99%

Core–shell microencapsulation of curcumin in PLGA microparticles: programmed for application in ovarian cancer therapy

Dwivedi

Yuan

Han

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

Self Cite

View full text Add to dashboard Cite

show abstract

“…In spite of these merits, CU suffers from its poor aqueous solubility, which in turn results in low bioavailability. CU complexed with phospholipids and its liposomes has also been evaluated to improve its oral bioavailability (10).…”

Section: Introductionmentioning

confidence: 99%

Cytotoxicity and Genotoxicity in Human Embryonic Kidney Cells Exposed to Surface Modify Chitosan Nanoparticles Loaded with Curcumin

et al. 2015

View full text Add to dashboard Cite

Abstract. The rapid progress in the development and scientific investments of modified nanoparticles are due to their owed activity to various diseased conditions for which they are prepared. But the toxicity which they cause cannot be overlooked. The present study demonstrates the development of phosphatidylserine (PS)-coated chitosan (CS) nanoparticles (NPs) loaded with curcumin (CU), which was then investigated against human embryonic kidney cells (HEK 293) for its cytotoxic and genotoxic effect in rats. The CU-loaded CNPs (CNPs-CU) have been prepared by ionic gelation method, later which were grafted with PS. CNPs-CU and PS-CNPs-CU have been evaluated for their size, poly dispersity index, amount of drug entrapped, and in vitro CU release. CNPs-CU has an average size 167.6 ± 3.53 nm and polydispersity index (PDI) 0.115 ± 0.014, whereas PS-CNPs-CU shows average size 220 ± 3.67 nm and PDI 0.148 ± 0.019. Surface morphology of prepared NPs was confirmed by high-resolution transmission electron microscopy (HR-TEM). There was no major difference in cell viability between PS-CNPs-CU and CNPs-CU when they were exposed to HEK 293 cells at all equivalent concentrations. A series of genotoxic studies were conducted, which revealed the non-genotoxicity potential of the developed complexes. These results demonstrated that PS-CNPs-CU may be useful as potential delivery system.

show abstract

“…Phospholipids are amphiphilic molecules, able to work as a surfactant to enhance the solubility of poorly water soluble drugs, but also as a carrier to improve the permeability of low membrane penetrating drugs. Examples of poorly water soluble drugs such as silybin, curcumin, hydroxycamptothecin, and naringenin have previously been formulated with phospholipids, and have shown excellent physicochemical properties and potentially higher therapeutic efficacies than their APIs. This has also been demonstrated for poorly oil‐soluble dugs, where Ruan et al formulated a matrine–phospholipid complex to improve liposolubility for a subsequent self‐emulsification formulation.…”

Section: Introductionmentioning

confidence: 99%

Phospholipid Complex of ICA and ICA II Prepared by Wet Media Milling for Improving Bioavailability

Pan

Cao

Tang

et al. 2018

Euro J Lipid Sci & Tech

View full text Add to dashboard Cite

In order to enhance the lipophilicity and thus oral bioavailability of icariin (ICA) and icariside II (ICA II) of total flavonoids of epimedium (TFE), a total flavonoids of epimedium–phospholipid complex (TFE‐PLC) is prepared by wet media milling. The stabilizers Aerosi and SDS are used to formulate TFE‐PLC nanosuspensions (TFE‐PLC–Ns) to improve the dispersion of TFE–PLC. FTIR and DSC data confirms the formation of TFE‐PLC. The oil solubility of ICA and ICA II in the complex in octanol is improved nearly four times over that in TFE. The logP of ICA in TFE‐PLC is significantly increased with a value from 1.61 to 2.02 at pH 4.5, and ICA II, from 3.24 to 4.77. The mean diameter of the TFE‐PLC‐Ns is reduced from 6.166 to 0.424 μm, and its dissolution is improved over TFE. In the in vivo evaluation, TFE‐PLC‐Ns exhibits a considerable enhancement with larger AUC0–t and shorter Tmax than TFE and TFE‐PLC. The relative bioavailability of ICA in TFE‐PLC and TFE‐PLC‐Ns are 181.75 and 249.05%, respectively, and for ICA II are 401.63 and 684.70%, respectively. Therefore, it suggests that TFE‐PLC‐Ns has possibilities in enhancing oral bioavailability of TFE, which may be due to its improved lipophilicity and wettability. Practical Applications: The oral bioavailability of ICA and ICA II in TFE are very low due to their poor lipophilicity and cell permeability. Here, TFE‐PLC‐Ns is proposed, which is prepared by wet media milling for improving lipophilic properties and oral bioavailability. In addition, some proofs of TFE‐PLC are investigated in detail, and TFE‐PLC‐Ns significantly increased the oral bioavailability of ICA and ICA II in TFE. Therefore, the authors recommend a potential drug vehicle of TFE‐PLC‐Ns for oral administration of ICA and ICA II, and a novel method of phospholipid complex preparation for industrial manufacture. In this article, the total flavonoids of epimedium–phospholipid complex (TFE‐PLC) is prepared to enhance the lipophilicity of icariin (ICA) and icariside II (ICA II) in TFE. Aerosi and SDS are used to formulate TFE‐PLC nanosuspensions (TFE‐PLC‐Ns) to improve the dispersion of TFE‐PLC. And finally, TFE‐PLC‐Ns exhibits enhanced oral bioavailability of ICA and ICA II compared with them in TFE and TFE‐PLC.

show abstract

Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

Cited by 30 publications

References 36 publications

Core–shell microencapsulation of curcumin in PLGA microparticles: programmed for application in ovarian cancer therapy

Core–shell microencapsulation of curcumin in PLGA microparticles: programmed for application in ovarian cancer therapy

Cytotoxicity and Genotoxicity in Human Embryonic Kidney Cells Exposed to Surface Modify Chitosan Nanoparticles Loaded with Curcumin

Phospholipid Complex of ICA and ICA II Prepared by Wet Media Milling for Improving Bioavailability

Contact Info

Product

Resources

About