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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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Journal ArticleDOI
TL;DR: The estimation of Lovastatin produced by Monascus purpureus and pure lovastatin was attempted by UV-visible spectrophotometer as well as HPLC, and HPLC analysis consistently gave reliable results for the estimation of lovastsatin under all the experimental conditions studied.
Abstract: Development of a novel method for the quantification of lovastatin is an interesting problem in the analytical field. In the literature, many reports use spectrophotometric method for the quantification of lovastatin. However, the analysis of fermentation broth containing lovastatin appears to be inaccurate using spectrophotometric method. Hence, the estimation of lovastatin produced by Monascus purpureus and pure lovastatin was attempted by UV-visible spectrophotometer as well as HPLC. It was observed that the analogues and/or intermediates of lovastatin synthesized in the fermentation broth and the products of fermentation caused superimposition effect on the absorption spectrum. Phosphate is a medium constituent for the production of lovastatin by the organism which contributed significantly to the superimposition of absorption spectrum. On the other hand, HPLC analysis consistently gave reliable results for the estimation of lovastatin under all the experimental conditions studied.

10 citations

Journal ArticleDOI
TL;DR: The importance of developing novel formulations of zerumbone to overcome its biopharmaceutical challenges thereby advance its potential in the treatment of various diseases is provided.
Abstract: About 40-70% of drug molecules in the clinical development pipeline suffer from one of either low aqueous solubility, poor absorption, or extremely low bioavailability. Approximately 75% of the world population relies on traditional therapies and therefore there has been a growing interest in the utilization of natural compounds. Zerumbone is one such natural compound, classified as a sesquiterpenoid that is extracted from the essential volatile oils of rhizomes from Zingiber zerumbet. It possesses strong antitumor, antioxidant, antimicrobial, and anti-inflammatory activity. However, despite promising preclinical studies demonstrating the therapeutic utility of zerumbone, its clinical development has been limited due to its low aqueous solubility, poor absorption, or associated low bioavailability. Multiple reviews demonstrating the pharmacological effects of zerumbone for various diseases have been published. However, to our knowledge, no review demonstrates the various formulation strategies developed to overcome the biopharmaceutical challenges of zerumbone. The purpose of this review is to provide a comprehensive perspective on zerumbone as a molecule for formulation development. A section related to pharmacokinetics, toxicity, and patents of zerumbone is included. This review provides the importance of developing novel formulations of zerumbone to overcome its biopharmaceutical challenges thereby advance its potential in the treatment of various diseases.

8 citations

Journal ArticleDOI
TL;DR: Lovastatin is the first FDA-approved antihypercholesterolemic drug for the treatment of cardiovascular diseases with pleiotropic clinical applications and Monascus purpureus is one of the safest molds for the production of lovastatin.
Abstract: Lovastatin is the first FDA-approved antihypercholesterolemic drug for the treatment of cardiovascular diseases with pleiotropic clinical applications. Monascus purpureus is one of the safest molds for the production of lovastatin that has been used in the preparation of Chinese medicine Red-Yeast Rice. This investigation dealt with the effect of both static and dynamic culture conditions on the morphological change and localization of lovastatin in Monascus purpureus. In dynamic culture condition, pellet morphology was observed and the maximum intra- and extra-cellular components of lovastatin including both β-hydroxy acid and lactone forms were found to be 1043.45 and 207.94 μg/l, respectively. Filamentous (mat) form of morphology was observed in the static culture condition and the intra- and extracellular concentration of lovastatin were 677.9 and 789.2 μg/l. Taguchi’s L12 (112) orthogonal arrays was employed to find optimal conditions for the submerged production of lovastatin and for the growth of Monascus purpureus. Three physical and five chemical variables were considered in the current experimental study. The maximum production of lovastatin was observed to be 3.66 mg/l. Among the chemical parameters, MnSO4 and MgSO4 were the most significant parameters for the production of lovastatin. Physical parameters, viz., agitation rate and temperature, were also equally significant to that of medium constituents for the production of lovastatin. The significance of the variables on the biomass growth was just opposite to that the results of lovastatin production. Ammonium chloride was the most significant parameter among the variables studied for the growth of M. purpureus, followed by glucose and phosphorous sources (KH2PO4). Statistical analysis showed that those parameters were significant with more than 99 % confidence (p<0.01).

8 citations


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

  • ...Indian Journal of Pharmaceutical Sciences 87 January-February 2018 Suitable statistical and/or non-statistical tools were employed to design the experiments and analysis the data for the optimization experiments[30-32]....

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  • ...However, these individual forms have different physico-chemical and pharmaceutical properties[30]....

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Patent
30 Jan 2014
TL;DR: In this article, compositions comprising inorganic oxide porous material containing a biologically active ingredient in liquid form, methods of making such compositions, and methods of using them are discussed. But the present paper is not concerned with the use of such compositions in the biomedical field.
Abstract: Compositions containing a biologically active ingredient and an inorganic oxide material are disclosed. Methods of making and using compositions containing a biologically active ingredient and an inorganic oxide material are also disclosed. The present invention relates to compositions comprising inorganic oxide porous material containing a biologically active ingredient in liquid form, methods of making such compositions, and methods of using them.

3 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....

    [...]

  • ...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....

    [...]