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Journal ArticleDOI

Lovastatin Nanoparticle Synthesis and Characterization for Better Drug Delivery

TL;DR: Nano drug delivery system is the latest technology employed in various medicinal applications and NLCs are a smarter generation of drug delivery carriers for lovastatin, a important drug which arrests the rate-limiting step of the cholesterol cascade.
Abstract: Nano drug delivery system is the latest technology employed in various medicinal applications. This technol- ogy can be adapted to the conventional drug administration due to its site-specific targeting phenomena. The oral lipo- philic drug administration has its drawbacks due to poor solubility and bioavailability. Lipid-based carrier systems are now widely popular due to improved efficiency, especially for lovastatin delivery. Lovastatin is an important drug which arrests the rate-limiting step of the cholesterol cascade. This drug has short half-lives, poor oral-administered bioavailabil- ity, poor solubility, and is rapidly metabolizable. Based on the composition, the drug delivery carriers are classified into solid lipid nanoparticles (SLNs), lipid emulsions (LEs), and nanostructured lipid carriers (NLCs). Among them, NLCs are a smarter generation of drug delivery carriers for lovastatin. The selection of various lipid systems and their formulation are discussed in this paper. Moreover, the characterization of these carrier systems to achieve the optimal characteristic features is discussed in a concise manner.

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Citations
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Journal ArticleDOI
TL;DR: Zerumbone-loaded nanostructured lipid carriers (ZER-NLC) have potential as a sustained-release drug carrier system for the treatment of leukemia, according to physicochemical properties.
Abstract: Zerumbone, a natural dietary lipophilic compound with low water solubility (1.296 mg/L at 25°C) was used in this investigation. The zerumbone was loaded into nanostructured lipid carriers using a hot, high-pressure homogenization technique. The physicochemical properties of the zerumbone-loaded nanostructured lipid carriers (ZER-NLC) were determined. The ZER-NLC particles had an average size of 52.68 ± 0.1 nm and a polydispersity index of 0.29 ± 0.004 μm. Transmission electron microscopy showed that the particles were spherical in shape. The zeta potential of the ZER-NLC was −25.03 ± 1.24 mV, entrapment efficiency was 99.03%, and drug loading was 7.92%. In vitro drug release of zerumbone from ZER-NLC was 46.7%, and for a pure zerumbone dispersion was 90.5% over 48 hours, following a zero equation. Using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay in human T-cell acute lymphoblastic leukemia (Jurkat) cells, the half maximal inhibitory concentration (IC50) of ZER-NLC was 5.64 ± 0.38 μg/mL, and for free zerumbone was 5.39 ± 0.43 μg/mL after 72 hours of treatment. This study strongly suggests that ZER-NLC have potential as a sustained-release drug carrier system for the treatment of leukemia.

116 citations


Cites background from "Lovastatin Nanoparticle Synthesis a..."

  • ...Approximately 40% of drugs in the pipeline and 70% of synthetic therapeutic molecules are plagued with poor solubility, oral bioavailability, and delivery.(8,9) Drugs with poor solubility suffer from limited transport after oral administration because of a low concentration gradient between the gut and blood vessels....

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Journal ArticleDOI
TL;DR: Crystals obtained from nitromethane solutions were found to have a very large reduction in aspect ratio to a prismatic morphology reflecting this solvent's propensity to interact with hydrophobic surfaces, critically with no polymorph change.

27 citations

Journal ArticleDOI
TL;DR: The importance and role of various nanoparticulate systems as carrier for antihyperlipidemic drugs in the treatment of hyperlipidemia and the development of efficient delivery methods and carriers are focused on.
Abstract: Hyperlipidemia is a prevailing risk factor that leads to development and progression of atherosclerosis and consequently cardiovascular diseases. Several antihyperlipidemic drugs are having various disadvantages such as low water solubility and poor bioavailabilty due to presystemic gastrointestinal clearance. Thus, there is a considerable need for the development of efficient delivery methods and carriers. This review focuses on the importance and role of various nanoparticulate systems as carrier for antihyperlipidemic drugs in the treatment of hyperlipidemia. Some nanoparticle technology-based products are approved by FDA for effective treatment of hyperlipidemia, namely Tricor® by Abbott Laboratories (Chicago, IL, USA) and Triglide® by Skye Pharma (London, UK). Efforts to address each of these issues are going on, and should remain the focus on the future studies and look forward to many more clinical products in the future.

26 citations


Cites background from "Lovastatin Nanoparticle Synthesis a..."

  • ...The nano-aided drug delivery system is a suitable choice for poorly soluble lipophilic drugs (Seenivasan et al., 2011)....

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Journal ArticleDOI
TL;DR: In vivo pharmacodynamics studies showed that the optimized LOV-s-rHDL displayed the most pronounced anti-atherosclerotic effect on decreasing plaque area and reducing the MMP level following an 8-week dosing regimen.
Abstract: Reconstituted high density lipoprotein (rHDL) is a biomimetic nanoparticle with plaque targeting and anti-atherosclerotic efficacy. In this work, we report on a strategy to rational design of lovastatin (LOV)-loaded spherical rHDL (LOV-s-rHDL) for efficient and safe anti-atherosclerotic therapy. Briefly, three LOV-s-rHDLs were formulated with LOV/s-rHDL at ratios of 8:1, 10:1, and 15:1 upon their respective median-effect values (Dm). The combined inhibitory effect between LOV and s-rHDL of different LOV-s-rHDL formulations on DiI-labeled oxLDL internalization was systemically investigated in RAW 264.7 cells based on the median-effect principle. Median-effect analysis demonstrated that the optimized LOV-s-rHDL was formulated with a ratio of 10:1 (Dm LOV:Dm s-rHDL), in which LOV and s-rHDL carrier showed the best synergistic effect, presumably ascribed to their inhibitory effect on CD36 and SR-A expression according to the Western blot analysis. In vivo pharmacodynamics studies showed that the optimized LOV...

18 citations

Journal ArticleDOI
TL;DR: Drug dissolution under non-digesting intestinal conditions revealed a three- to sixfold increase in dissolution efficiencies when compared to the unformulated drug and a LOV-lipid suspension, and the SSL-S provided superior drug solubilization under simulated intestinal digesting condition.
Abstract: Low dissolution of drugs in the intestinal fluid can limit their effectiveness in oral therapies. Here, a novel porous silica-supported solid lipid system was developed to optimize the oral delivery of drugs with limited aqueous solubility. Using lovastatin (LOV) as the model poorly water-soluble drug, two porous silica-supported solid lipid systems (SSL-A and SSL-S) were fabricated from solid lipid (glyceryl monostearate, GMS) and nanoporous silica particles Aerosil 380 (silica-A) and Syloid 244FP (silica-S) via immersion/solvent evaporation. SSL particles demonstrated significantly higher rate and extent of lipolysis in comparison with the pure solid lipid, depending on the lipid loading levels and the morphology. The highest lipid digestion was observed when silica-S was loaded with 34% (w/w) solid lipid, and differential scanning calorimeter (DSC) analysis confirmed the encapsulation of up to 2% (w/w) non-crystalline LOV in this optimal SSL-S formulation. Drug dissolution under non-digesting intestinal conditions revealed a three- to sixfold increase in dissolution efficiencies when compared to the unformulated drug and a LOV-lipid suspension. Furthermore, the SSL-S provided superior drug solubilization under simulated intestinal digesting condition in comparison with the drug-lipid suspension and drug-loaded silica. Therefore, solid lipid and nanoporous silica provides a synergistic effect on optimizing the solubilization of poorly water-soluble compound and the solid lipid-based porous carrier system provides a promising delivery approach to overcome the oral delivery challenges of poorly water-soluble drugs.

10 citations

References
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Journal ArticleDOI
TL;DR: The biological activity of parenterally applied SLN and biopharmaceutical aspects such as pharmacokinetic profiles as well as toxicity aspects are reviewed.

1,302 citations


"Lovastatin Nanoparticle Synthesis a..." refers background in this paper

  • ...This paper discusses emerging formulation designs for the delivery of poorly water-soluble lovastatin, their characterization, and applications....

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  • ...Carrier development for the parenteral administration of these drugs has many problems including the massive use of surface-active excipients for solubilization [1]....

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  • ...These systems demand suitable conditions for drug delivery, viz., the use of physiologically tolerated lipids, large-scale production, protection of drugs from degradation, improved bioavailability, minimum level of toxicity, and controlledrelease characteristics....

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Journal ArticleDOI
TL;DR: An overview of the cosmetic products currently on the market is given and the improvement of the benefit/risk ratio of the topical therapy is shown and the lipid nanoparticles are a "nanosafe" carrier.

1,186 citations


Additional excerpts

  • ...Keywords: Lovastatin, nanoparticles, solid lipid nanoparticles, lipid emulsions, nano-structured lipid carriers....

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Journal ArticleDOI
TL;DR: This review will primarily focus on the recent advances and updates on lipid-based nanoparticles for their projected applications in drug delivery, including a review of current activities in the field of liposomes, and challenging issues of targeting and triggering will be discussed in detail.
Abstract: In recent years, various nanotechnology platforms in the area of medical biology, including both diagnostics and therapy, have gained remarkable attention. Moreover, research and development of engineered multifunctional nanoparticles as pharmaceutical drug carriers have spurred exponential growth in applications to medicine in the last decade. Design principles of these nanoparticles, including nano-emulsions, dendrimers, nano-gold, liposomes, drug-carrier conjugates, antibody-drug complexes, and magnetic nanoparticles, are primarily based on unique assemblies of synthetic, natural, or biological components, including but not limited to synthetic polymers, metal ions, oils, and lipids as their building blocks. However, the potential success of these particles in the clinic relies on consideration of important parameters such as nanoparticle fabrication strategies, their physical properties, drug loading efficiencies, drug release potential, and, most importantly, minimum toxicity of the carrier itself. Among these, lipid-based nanoparticles bear the advantage of being the least toxic for in vivo applications, and significant progress has been made in the area of DNA/RNA and drug delivery using lipid-based nanoassemblies. In this review, we will primarily focus on the recent advances and updates on lipid-based nanoparticles for their projected applications in drug delivery. We begin with a review of current activities in the field of liposomes (the so-called honorary nanoparticles), and challenging issues of targeting and triggering will be discussed in detail. We will further describe nanoparticles derived from a novel class of amphipathic lipids called bolaamphiphiles with unique lipid assembly features that have been recently examined as drug/DNA delivery vehicles. Finally, an overview of an emerging novel class of particles (based on lipid components other than phospholipids), solid lipid nanoparticles and nanostructured lipid carriers will be presented. We conclude with a few examples of clinically successful formulations of currently available lipid-based nanoparticles.

768 citations


"Lovastatin Nanoparticle Synthesis a..." refers background in this paper

  • ...Lovastatin, a cholesterol-lowering agent, is isolated from strains such as Aspergillus, Monascus, and Streptomycetes species....

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  • ...The potential problems associated with conventional oraladministrated system (tablets) are non-specific targeting, side effects due to high dosage, and poor stability....

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  • ...Keywords: Lovastatin, nanoparticles, solid lipid nanoparticles, lipid emulsions, nano-structured lipid carriers....

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Journal ArticleDOI
TL;DR: The article gives an overview of the cosmetic benefits of lipid nanoparticles, that means enhancement of chemical stability of actives, film formation, controlled occlusion, skin hydration, enhanced skin bioavailability and physical stability of the lipid nanoparticle as topical formulations.

603 citations


"Lovastatin Nanoparticle Synthesis a..." refers background in this paper

  • ...This paper discusses emerging formulation designs for the delivery of poorly water-soluble lovastatin, their characterization, and applications....

    [...]

  • ...Keywords: Lovastatin, nanoparticles, solid lipid nanoparticles, lipid emulsions, nano-structured lipid carriers....

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  • ...Hence, this compound is encapsulated or coated with a suitable carrier to enhance its bioavailability and other properties, viz., dissolution rate, half-life period, drug loading capacity, and maximum attainable plasma concentration....

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  • ...Another important parameter is lipophilicity which determines the nature of the diffusion system....

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  • ...However, the oral administration of this drug has certain limitations, viz., poor bioavailability, nonhepatic shunting, side effects due to higher dosage, more excretion in bile....

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Journal ArticleDOI
TL;DR: The barriers to CNS drug delivery, strategies to bypass the blood-brain barrier and characterization methods of SLNs and their usefulness are discussed.

523 citations


Additional excerpts

  • ...Keywords: Lovastatin, nanoparticles, solid lipid nanoparticles, lipid emulsions, nano-structured lipid carriers....

    [...]