Lipid nanocapsules: A new platform for nanomedicine (original) (raw)

Lipid nanocapsules for intracellular drug delivery of anticancer drugs

Journal of nanoscience and nanotechnology, 2007

As non-phagocytic eukaryotic cells can internalize particles < 1 microm in size, small size (25 to 110 nm) lipid nanocapsules (LNC) are proposed for the intracellular drug delivery of anticancer drugs to cancer cells. LNC of different diameters were loaded with etoposide or paclitaxel and subsequently tested for drug release kinetics and their efficiency to reduce cancer cell growth in cell culture. Relative high drug loads could be achieved and sustained drug release can be provided over a period of several days (etoposide) up to a few weeks (paclitaxel). While particle size exhibited only minor influences on the release kinetics, higher initial drug load led to a distinctly lower burst release. In a cancer cell culture model, etoposide or paclitaxel LNC showed a 4-fold or 40-fold higher efficiency, respectively than the drug solution while blank LNC were found to be less toxic than the pure drug at equivalent concentrations. The uptake and intracellular accumulation of LNC was ...

Novel Long-Circulating Lipid Nanocapsules

Pharmaceutical Research, 2004

Purpose. To develop and evaluate novel long-circulating lipid nanocapsules (LN) designed for tumor delivery of lipophilic drugs. Methods. Nanocapsules were produced by a solvent-free phase inversion process and were coated with polyethylene glycoldistearoylphosphatidylethanolamine conjugate (DSPE-PEG) during preparation or by a post-insertion step. In vivo studies were conducted in rats to assess LN pharmacokinetics and biodistribution. Results. Post-insertion of DSPE-PEG appeared to be a convenient and effective method of obtaining LN of controlled sizes with high PEG density at their surface. After intravenous injection to rats, PEGylated lipid nanocapsules obtained by the post-insertion method exhibited long-circulating properties. Up to 50% of the injected dose was still present in the blood 8 h after administration for LN containing 6 mol% PEG 5000 or 10 mol% PEG 2000. This represented an area under the blood concentration-time curve of almost 70% that of liposomes used in the Doxil formulation. Conclusion. With a simple solvent free-process, it was possible to produce long-circulating LN of controlled sizes. Such LN could prove useful for the passive delivery of lipophilic anticancer drugs to solid tumors.

Combinational drug-loaded lipid nanocapsules for the treatment of cancer

International Journal of Pharmaceutics, 2019

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Nanostructured Lipid Carriers: A Novel Platform for Chemotherapeutics

Cancer is a disease manifested as abnormal cells division without control. If it is not detected and cured very timely, it can invade other healthy tissues resulting in metastasis. Chemotherapy is the first line treatment for cancer, but due to lack of specificity of most of the anticancer drugs, is associated with side effects that affect the quality of life. Nanostructured lipid carriers (NLC) are one of the promising nano-carriers for the development of effective targeted therapies for cancer chemothera-peutics. These bio-compatible and/or biodegradable lipids based nanoparticles are composed of solid and liquid lipids as a core matrix dispersed in surfactant solution. NLC improve the aqueous solubility of most of the hydrophobic cancer therapeutics. Their surface modification can be used for overcoming drug resistance in cancer chemotherapy, to achieve site specific targeting for better efficacy and reduced dose related toxicity. The present review is an attempt to contemplate their pharmaceutical, biopharmaceutical aspects and application in cell targeting, gene delivery and in theranostics.

Characterization of Different Functionalized Lipidic Nanocapsules as Potential Drug Carriers

International Journal of …, 2012

Lipid nanocapsules (LNC) based on a core-shell structure consisting of an oil-filled core with a surrounding polymer layer are known to be promising vehicles for the delivery of hydrophobic drugs in the new therapeutic strategies in anti-cancer treatments. The present work has been designed as basic research about different LNC systems. We have synthesized-and physico-chemically characterized-three different LNC systems in which the core was constituted by olive oil and the shell by different phospholipids (phosphatidyl-serine or lecithin) and other biocompatible molecules such as Pluronic ® F68 or chitosan. It is notable that the olive-oil-phosphatidyl-serine LCN is a novel formulation presented in this work and was designed to generate an enriched carboxylic surface. This carboxylic layer is meant to link specific antibodies, which could facilitate the specific nanocapsule uptake by cancer cells. This is why nanoparticles with phosphatidyl-serine in their shell have also been used in this work to form immuno-nanocapsules containing a polyclonal IgG against a model antigen (C-reactive protein) covalently bounded by means of a simple and reproducible carbodiimide method. An immunological study was made to verify that these IgG-LNC complexes showed the expected specific immune response. Finally, a preliminary in vitro study was performed by culturing a breast-carcinoma cell line (MCF-7)

In vivo evaluation of lipid nanocapsules as a promising colloidal carrier for paclitaxel

International Journal of Pharmaceutics, 2007

Paclitaxel-loaded lipid nanocapsules (PX-LNC) exhibit interesting in vitro characteristics with improved antitumoral activity compared with free PX formulation. Biodistribution studies were realized with the use of 14 C-trimyristin ( 14 C-TM) or 14 C-phosphatidylcholine ( 14 C-PC) whereas antitumoral activity of PX-LNC formulations was based on the animal survival in a chemically induced hepatocellular carcinoma (HCC) model in Wistar rats. Blood concentration-time profiles for both labeled 14 C-TM-LNC and 14 C-PC-LNC were similar; the t 1/2 and MRT values (over 2 h and close to 3 h, respectively, for both formulations) indicated the long circulating properties of the LNC carrier with a slow distribution and elimination phase. Survival curves of paclitaxel treated groups showed a statistical significant difference compared to the control survival curve (P = 0.0036 and 0.0408). Animals treated with 4× 70 mg/m 2 of PX-LNC showed the most significant increase in mean survival times compared to the controls (IST mean 72%) and cases of long-term survivors were preferentially observed in the PX-LNC treated group (37.5%; 3/8). These results demonstrate the great interest to use LNC as drug delivery system for paclitaxel, permitting with an equivalent therapeutic efficiency to avoid the use of excipients such as polyoxyethylated castor oil for its formulation.

Antineoplastics Encapsulated in Nanostructured Lipid Carriers

Molecules, 2021

Ideally, antineoplastic treatment aims to selectively eradicate cancer cells without causing systemic toxicity. A great number of antineoplastic agents (AAs) are available nowadays, with well-defined therapeutic protocols. The poor bioavailability, non-selective action, high systemic toxicity, and lack of effectiveness of most AAs have stimulated the search for novel chemotherapy protocols, including technological approaches that provide drug delivery systems (DDS) for gold standard medicines. Nanostructured lipid carriers (NLC) are DDS that contain a core of solid and lipid liquids stabilised by surfactants. NLC have high upload capacity for lipophilic drugs, such as the majority of AAs. These nanoparticles can be prepared with a diversity of biocompatible (synthetic or natural) lipid blends, administered by different routes and functionalised for targeting purposes. This review focused on the research carried out from 2000 to now, regarding NLC formulations for AAs (antimetabolite...

Drug Encapsulated Lipid-Polymeric Nanohybrid as a Chemo-therapeutic Platform of Cancer

Nanotheranostics

The focus of this research is to design a bioengineered drug delivery vehicle that is efficient in anti-cancer drug delivery in a controlled manner. The experimental work focuses on constructing a methotrexateloaded nano lipid polymer system (MTX-NLPHS) that can transport methotrexate (MTX) in MCF-7 cell lines in a controlled manner through endocytosis via phosphatidylcholine. In this experiment, MTX is embedded with polylactic-co-glycolic acid (PLGA) in phosphatidylcholine, which acts as a liposomal framework for regulated drug delivery. Scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and dynamic light scattering (DLS) were utilized to characterize the developed nanohybrid system. The particle size and encapsulation efficiency of the MTX-NLPHS were found to be 198 ± 8.44 nm and 86.48 ± 0.31 %, respectively, which is suitable for biological applications. The polydispersity index (PDI) and zeta potential of the final system were found to be 0.134 ± 0.048 and-28 ± 3.50 mV, respectively. The lower value of PDI showed the homogenous nature of the particle size, whereas higher negative zeta potential prevented the system from agglomeration. An in vitro release kinetics was conducted to see the release pattern of the system, which took 250 h for 100% drug release This kind of system may carry the drug for a long time in the circulatory system and prevent the drug discharge. Other cell culture assays such as 3-(4, 5-dimethyl thiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) and reactive oxygen species (ROS) monitoring were used to see the effect of inducers on the cellular system. MTT assay showed cell toxicity of MTX-NLPHS reduced at the lower concentration of the MTX, however, toxicity increased at the higher concentration of the MTX as compared to free MTX. ROS monitoring c revealed more scavenging of ROS using MTX-NLPHS as compared to free MTX. Confocal microscopy suggested the MTX-NLPHS induced more nuclear elongation with cell shrinkage comparatively.

LIPID BASED NANOPARTICLES IN CANCER THERAPY

Indo American Journal of Pharmaceutical Research, 2023

Investigators were continuously creating novel nanotechnologies to address unmet requirements throughout the administration of therapeutic medicines & imaging agents for cancer treatment & diagnostics, appropriately. LNPs (Lipid nanoparticles) are legitimate particulates (approx. 100 nm in size) gathered from various lipid as well as other biochemical compounds which overall functionality to resolve biological barriers (bioba rriers), allowing LNPs to selectively collect somewhere outside of disease-target cells again for responsive therapeutics. Most pharmaceutically important compounds were insoluble throughout water solutions, were chemical & physiologically unstable, or have toxicities. Among the most potential drug carrier for bioactive organic compounds is LBNPs (Lipid based nanoparticles) technologies. Its present use in chemotherapy has transformed treatment for cancer by increasing the antitumor effect of a number of chemotherapeutics. Because they may be created using naturally occurring sources, LBNPs have great temporal and thermal stability, maximum load potential, simplicity of preparations, cheap manufacturing costs, & big manufacturing output. Furthermore, combining chemotherapeutic drugs with LNPs reduces active therapeutic dosage and toxicities, lowers treatment resistance, & raises drug concentration in tumour cells while reducing concentrations in normal tissue. LBNPs were widely studied in cancer treatment, both in vitro and in vivo, with encouraging outcomes in certain clinical trials. This study provides an overview of the many types of LBNPs which have been created in latest years and their applications and contributions in different types of cancers.