Development of a Respirable, Sustained Release Microcarrier for 5-Fluorouracil I: In Vitro Assessment of Liposomes, Microspheres, and Lipid Coated Nanoparticles

Hitzman, Cory J.; Elmquist, William F.; Wattenberg, Lee W.; Wiedmann, Timothy S.

doi:10.1002/jps.20591

Cited by 96 publications

(63 citation statements)

References 26 publications

(32 reference statements)

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“…5-FU SLNs prepared using phospholipids were found to effectively reduce MDA-MB-468 tumor growth [9]. As an inhalation therapy, 5-FU SLNs have been found effective in lung cancer [10,11]. Multiple emulsion-ultrasonication method has also been employed to prepare 5-FU, which was found to be a promising alternative for passive targeting therapeutic agents for curing primary lung carcinoma [12].…”

mentioning

confidence: 99%

In vitro anticancer evaluation of 5-fluorouracil lipid nanoparticles using B16F10 melanoma cell lines

Shenoy

Gude²,

Murthy

2013

Int Nano Lett

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The present study is aimed to investigate the formulation and in vitro anticancer activities of solid lipid nanoparticles (SLNs) of 5-fluorouracil (5-FU) prepared using glyceryl monostearate (GMS) and cetyl palmitate (CP) by hot homogenization method. The lipids were selected based on the partition coefficient of 5-FU in lipids. The lipid nanoparticles were optimized for process and formulation parameters. The optimized nanoparticles were characterized for their zeta potential, morphology, release kinetics, and anticancer activity. Higher entrapments were achieved using a combination of emulsifiers. The zeta potential of the optimized CP and GMS SLN formulation were −8.26 and −9.35 mV, respectively. Both the optimized formulations were spherical. The in vitro release studies of SLNs of both the lipid carriers followed Peppas-Korsenmeyer equation when carried out at pH 3.5 and 7.4. The chemosensitivity assay carried out in B16F10 cell lines revealed that CP SLNs had better cytotoxicity than 5-FU solution and GMS SLNs at 48 h of incubation. Subtoxic concentration of 5-FU-loaded CP SLNs (0.12 μg/mL) possessed comparable antimigrational activity, colony inhibition activity, and cytopathic as that of 5-FU solution effects. The results indicated that encapsulating 5-FU in CP would be a promising delivery system for delivering 5-FU.

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mentioning

confidence: 99%

In vitro anticancer evaluation of 5-fluorouracil lipid nanoparticles using B16F10 melanoma cell lines

Shenoy

Gude²,

Murthy

2013

Int Nano Lett

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“…However, this concept contradicts the fact that, due to blood circulation in the lung 52,53 and the lymphatic circulation, drug concentrations have been found in the systemic circulation and surgically resected lymph nodes. 31,32,84,131,230,231,238 In addition, a high percentage of lymph nodes in the aerosol treatment groups did not show any metastasis in several studies, so it is possible that this route of administration destroys tumor cells and prevents them from trafficking from the primary subcutaneous tumor to the lungs and lymph nodes via the lymphatic system. 31,32,49,57 Nevertheless, in many of these studies, an additional intravenous chemotherapy regimen was administered, so clear conclusions cannot be drawn.…”

Section: Resultsmentioning

confidence: 99%

“…Furthermore, an evaluation has to be made of whether inhaled chemotherapy is appropriate for early-stage lung cancer, or as neoadjuvant or adjuvant treatment. 57,60,61,230,231 Because lesions are of smaller size, drug deposition is not prevented by the large mass median diameter of the tumor. 131 Current drug delivery systems have demonstrated an ability to achieve sustained release locoregionally, but further improvement is welcomed.…”

Section: Resultsmentioning

confidence: 99%

“…60 Moreover, additional formulations of 5-FU with lipid-coated nanoparticles or difluoromethylornithine, an important enzyme in cell proliferation, were devised to achieve sustained drug release and enhance anticancer properties. 60,230,231 In these studies, previously presented for their inhalable system carriers with 5-FU, a step was made forward in using inhaled chemotherapy as an adjuvant treatment. Studies using taxanes either with liposome carriers, nanoparticles, polymeric micelles, or lipid nanocapsules provided evidence of an increased therapeutic index by prolonging regional action in the lung.…”

Section: Inhalation Studiesmentioning

confidence: 99%

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Inhaled chemotherapy in lung cancer: future concept of nanomedicine

Zarogoulidis

Chatzaki²,

Porpodis³

et al. 2012

IJN

166

160

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Regional chemotherapy was first used for lung cancer 30 years ago. Since then, new methods of drug delivery and pharmaceuticals have been investigated in vitro, and in animals and humans. An extensive review of drug delivery systems, pharmaceuticals, patient monitoring, methods of enhancing inhaled drug deposition, safety and efficacy, and also additional applications of inhaled chemotherapy and its advantages and disadvantages are presented. Regional chemotherapy to the lung parenchyma for lung cancer is feasible and efficient. Safety depends on the chemotherapy agent delivered to the lungs and is dose-dependent and time-dependent. Further evaluation is needed to provide data regarding early lung cancer stages, and whether regional chemotherapy can be used as neoadjuvant or adjuvant treatment. Finally, inhaled chemotherapy could one day be administered at home with fewer systemic adverse effects.

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“…Nanotechnology-based formulations in respiratory disorders are beneficial in many ways which involves: (1) Probably to attain consistent delivery of drug dose along with the alveolus (2) Acquisition of improved solubility of the active ingredient over its own water solubility (3) Continuous-release lowers the dose repetition of drug (4) Appropriate release of macromolecules (5) Decline in occurrence of adverse effects (6) Better patient compatibility and (7) Probable of drug internalization through cells (Bailey & Berkland, 2009) Initial new drug treatment to create a statistically endurance advantage above regular treatment is use of combination therapy of Vinorelbine or Vindesine and Cisplatin (Wozniak et al, 1998). Effectiveness of combination of Vinorelbine and cisplatin was proved for metastatic NSCLC (Hitzman et al, 2006). When cisplatin alone was used for 1 year, endurance was 20%; but, when used in combination, endurance was 36%.…”

Section: Treatment Strategiesmentioning

confidence: 99%

Surfactant-based drug delivery systems for treating drug-resistant lung cancer

et al. 2014

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Among all cancers, lung cancer is the major cause of deaths. Lung cancer can be categorized into two classes for prognostic and treatment purposes: small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC). Both categories of cancer are resistant to certain drugs. Various mechanisms behind drug resistance are over-expression of superficial membrane proteins [glycoprotein (P-gp)], lung resistance-associated proteins, aberration of the intracellular enzyme system, enhancement of the cell repair system and deregulation of cell apoptosis. Structure-performance relationships and chemical compatibility are consequently major fundamentals in surfactant-based formulations, with the intention that a great deal investigation is committed to this region. With the purpose to understand the potential of P-gp in transportation of anti-tumor drugs to cancer cells with much effectiveness and specificity, several surfactant-based delivery systems have been developed which may include microspheres, nanosized drug carriers (nanoparticles, nanoemulsions, stealth liposomes, nanogels, polymer-drug conjugates), novel powders, hydrogels and mixed micellar systems intended for systemic and/or localized delivery.

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Development of a Respirable, Sustained Release Microcarrier for 5-Fluorouracil I: In Vitro Assessment of Liposomes, Microspheres, and Lipid Coated Nanoparticles

Cited by 96 publications

References 26 publications

In vitro anticancer evaluation of 5-fluorouracil lipid nanoparticles using B16F10 melanoma cell lines

In vitro anticancer evaluation of 5-fluorouracil lipid nanoparticles using B16F10 melanoma cell lines

Inhaled chemotherapy in lung cancer: future concept of nanomedicine

Surfactant-based drug delivery systems for treating drug-resistant lung cancer

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