Studies on Development of Controlled Release Matrix Tablets of Camptothecin-An Anticancer Drug

Nalluri, Buchi N.; Devineni, Pavan Kumar; Male, Maheswari Karna; Shaik, Ashraf Sultana; Uppuluri, Chandra Teja

doi:10.5530/ijper.49.4s.5

Cited by 4 publications

(3 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…These bands correspond to νOH, carbonyl stretching of the cyclic ester (lactone), νCO (pyridone), νCC, and νCC(O)O, respectively. 53,54 These bands were also observed in the functionalized nanomaterials, which confirms the adsorption of CPT on the GO−CPT and GO−FA + CPT nanocarriers (Figure 2C).…”

Section: Resultssupporting

confidence: 64%

Folic-Acid-Functionalized Graphene Oxide Nanocarrier: Synthetic Approaches, Characterization, Drug Delivery Study, and Antitumor Screening

Sousa

Luna

Fonseca

et al. 2018

ACS Appl. Nano Mater.

View full text Add to dashboard Cite

In this work, we developed and screened the potential antitumor activity of a nanocarrier based on graphene oxide (GO) and folic acid (FA) for the delivery of chemotherapy drugs. GO was synthesized by the graphite exfoliation process. FA was linked to PEG (4,7,10-trioxa-1,13-tridecanediamine) to form FA–PEG, followed by coupling to the GO surface. Camptothecin (CPT) was further adsorbed on GO for use as a drug model in the delivery study. The synthesis of the intermediate FA–PEG molecule and coupling to GO for the formation of the GO–FA nanocarrier were confirmed by basic and state-of-the-art characterization techniques, including infrared (FTIR) spectroscopy, thermogravimetric analysis (TGA), electrospray ionization (ESI) mass spectrometry, transmission electron microscopy (TEM), and magic-angle spinning carbon-13 nuclear magnetic resonance (CP/MAS 13C NMR) spectroscopy. FTIR spectroscopy showed a significant reduction in the signal intensity of the carboxylic groups after the functionalization of GO with FA–PEG. TGA of GO–FA revealed that approximately 20% of the functional groups were from FA–PEG. GO–FA indicated a high CPT loading capacity (37.8%). In vitro studies confirmed prolonged drug release over 200 h. Acidic pH (5.0) slowed the release of CPT from the nanocarrier compared to that at physiological pH (7.4). The toxicity screening of GO–FA and GO–FA + CPT was investigated for two widely studied preclinical cell models: J774, a tumor cell with macrophage phenotype and high proliferation rate; and HepG2, a tumor cell obtained from human hepatocellular carcinoma with folate transporters. The toxicity of the GO–FA nanocarrier without drug loading was dependent on the cell type and presented no toxicity to J774 but high toxicity to HepG2. The presence of FA in the nanocarrier loaded with CPT was crucial to achieve apoptosis in both tumor cell lines. In addition, confocal microscopy revealed both the adhesion and internalization of the FITC-labeled GO–FA by the tumor cell lines.

show abstract

Section: Resultssupporting

confidence: 64%

Folic-Acid-Functionalized Graphene Oxide Nanocarrier: Synthetic Approaches, Characterization, Drug Delivery Study, and Antitumor Screening

Sousa

Luna

Fonseca

et al. 2018

ACS Appl. Nano Mater.

View full text Add to dashboard Cite

show abstract

“…Mass spectroscopy gives information about the molecular weight of the specific compound which is the most important confirmatory test for the identification of isolated moieties which exactly matches with the standard molecular weight of standard camptothecin. The mass spectra of camptothecin give precursor m/z peak at 349.2 [M+H]+ in plain, and the mass spectra match with the peak for standard camptothecin [34][35][36]. Results were shown in Fig.…”

Section: Mass Spectroscopymentioning

confidence: 76%

Design and characterization of camptothecin gel for treatment of epidermoid carcinoma

Galatage¹,

Hebalkar²,

Gote³

et al. 2020

Futur J Pharm Sci

View full text Add to dashboard Cite

Background: The objective of present research work is to design and characterize camptothecin gel using Carbopol-934 for the treatment of epidermoid carcinoma. Optimized herbal gel formulations were evaluated for homogeneity and appearance, viscosity, extrudability, spreadability, drug content, drug release, pH, and in vitro skin cancer activity on A431 cell lines. Results: Mass and Infrared Spectra respectively conforms molecular weight and functional groups present in camptothecin. All the formulations F1 to F5 showed good homogeneity, pH from 6.68 to 6.90, spreadability in the range of 15.81-23.37 gm.cm/s, extrudability 85.51-90.45% w/w, drug content 89.12-96.64%, and in vitro diffusion 88.36-98.40%, respectively. The drug release study showed that all the formulations followed a diffusion-controlled, zero-order release mechanism. Anticancer activity results indicate that camptothecin gel induce cell death in A-439 cells having IC 50 48.03 μg and % apoptosis 54.67 ± 4.58. Conclusion: Topical delivery of camptothecin alleviates the side effects caused by systemic chemotherapy; hence, the developed herbal gel formulation can be effectively useful to deliver camptothecin in the treatment of epidermoid carcinoma on A-431 cells.

show abstract

“…The in vitro release of CPT in the first 30 min was minimal, with only 7.4% of the total CPT drugs in NRs being released ( figure 3; solid line). The polymer coating began to disintegrate, releasing ∼40% of total CPT in 24 h and more than 50.8% in 72 h. A 100% drug release of CPT was limited by its low (∼10 μg ml −1 ) water solubility [60,61]. Galbiate et al measured 40% cumulative dissolution of CPT over 3 days from chitosan biopolymer coated microcapsules in PBS of pH 7.4 [62].…”

Section: Discussionmentioning

confidence: 99%

Bioresponsive polymer coated drug nanorods for breast cancer treatment

et al. 2016

View full text Add to dashboard Cite

Ineffective drug release at the target site is among the top challenges for cancer treatment. This reflects the facts that interaction with the physiological condition can denature active ingredients of drugs, and low delivery to the disease microenvironment leads to poor therapeutic outcomes. We hypothesize that depositing a thin layer of bioresponsive polymer on the surface of drug nanoparticles would not only protect drugs from degradation but also allow the release of drugs at the target site. Here, we report a one-step process to prepare bioresponsive polymer coated drug nanorods (NRs) from liquid precursors using the solvent diffusion method. A thin layer (10.3 ± 1.4 nm) of poly(ε-caprolactone) (PCL) polymer coating was deposited on the surface of camptothecin (CPT) anti-cancer drug NRs. The mean size of PCL-coated CPT NRs was 500.9 ± 91.3 nm length × 122.7 ± 10.1 nm width. The PCL polymer coating was biodegradable at acidic pH 6 as determined by Fourier transform infrared spectroscopy. CPT drugs were released up to 51.5% when PCL coating dissolved into non-toxic carboxyl and hydroxyl groups. Trastuzumab (TTZ), a humanized IgG monoclonal antibody, was conjugated to the NR surface for breast cancer cell targeting. Combination treatments using CPT and TTZ decreased the HER-2 positive BT-474 breast cancer cell growth by 66.9 ± 5.3% in vitro. These results suggest effective combination treatments of breast cancer cells using bioresponsive polymer coated drug delivery.

show abstract

Studies on Development of Controlled Release Matrix Tablets of Camptothecin-An Anticancer Drug

Cited by 4 publications

References 15 publications

Folic-Acid-Functionalized Graphene Oxide Nanocarrier: Synthetic Approaches, Characterization, Drug Delivery Study, and Antitumor Screening

Folic-Acid-Functionalized Graphene Oxide Nanocarrier: Synthetic Approaches, Characterization, Drug Delivery Study, and Antitumor Screening

Design and characterization of camptothecin gel for treatment of epidermoid carcinoma

Bioresponsive polymer coated drug nanorods for breast cancer treatment

Contact Info

Product

Resources

About