Formulation and Characterization of Nifedipine loaded Nanostructured Lipid Carriers coated with Fenugreek Seed Polysaccharide (original) (raw)
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The present study is aimed at preparation and development of Nanostructured lipid carriers from natural polysaccharide extracted from Tamarind seeds (Tamarindus indica) for the sustained delivery of Nifedipine. The Nifedipine loaded NLCs were prepared by solvent injection technique with the isolated tamarind seed polysaccharide. The formulations were optimized using two level factorial design using the polysaccharide, solid lipid and liquid lipid as independent variables and particle size (PS), drug entrapment efficiency as the dependent variables. The NLCs were characterized in terms of PS, entrapment efficiency, in vitro drug release and Scanning Electron Microscopy. Stable NLCs were obtained with average PS of 285.1 ± 4.6 nm. The entrapment efficiency of optimized batch was found to be 82.56 ± 2.5% (w/w). In vitro drug release showed controlled release pattern showing up to 90% release in 24 h. It may be concluded from the study that tamarind seed polysaccharides may be suitable for formulation of NLCs for better efficacy and sustained delivery of hypertensive drug Nifedipine.
Encapsulation and drug release of poorly water soluble nifedipine from bio-carriers
Journal of Non-Crystalline Solids, 2018
Controlled drug delivery is one of the most intruding field in pharmaceutical research. It is desired for most of the drugs due to safety and efficacy reasons. Another emerging field is improving the bioavailability of poorly water-soluble drugs. By encapsulating such drugs into biodegradable polysaccharide materials both, improved bioavailability and controlled drug release is readily expected. Nifedipine, used as a model drug, was encapsulated within polysaccharide gels by the novel ethanol induced gelation method. Wet materials were processed by supercritical technology to retain its form and structure. Swelling and in-vitro dissolution tests were performed to investigate the swelling of aerogels and release behavior of nifedipine within body fluids. It was observed that guar and xanthan are not the best candidates for oral delivery of nifedipine, since the release was prolonged to 14 days. Oppositely, pectin and alginate are both suitable for nifedipine encapsulation as they released 100% of nifedipine within the first 5 h. Higher drug loading was achieved by pectin aerogels most likely due to their higher surface area.
AAPS PharmSciTech, 2014
The aim of this study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of a lipid lowering agent, fenofibrate (FEN). FEN-loaded NLCs (FEN-NLCs) were prepared by hot homogenization followed by an ultrasonication method using Compritol 888 ATO as a solid lipid, Labrafil M 1944CS as a liquid lipid, and soya lecithin and Tween 80 as emulsifiers. NLCs were characterized in terms of particle size and zeta pote\ntial, surface morphology, encapsulation efficiency, and physical state properties. Bioavailability studies were carried out in rats by oral administration of FEN-NLC. NLCs exhibited a spherical shape with a small particle size (84.9±4.9 nm). The drug entrapment efficiency was 99% with a loading capacity of 9.93±0.01% (w/w). Biphasic drug release manner with a burst release initially, followed by prolonged release was depicted for in vitro drug release studies. After oral administration of the FEN-NLC, drug concentration in plasma and AUC t-∞ was fourfold higher, respectively, compared to the free FEN suspension. According to these results, FEN-NLC could be a potential delivery system for improvement of loading capacity and control of drug release, thus prolonging drug action time in the body and enhancing the bioavailability.
Formulation and Evaluation of Nifedipine Loaded Solid Lipid Nanoparticles
Asian Journal of Research in Chemistry and Pharmaceutical Sciences
INTRODUCTON Nifedipine (Dihydropyridine derivative) is calcium channel blocker. It is also a peripheral arterial vasodilator which acts on smooth muscle. It is used in the treatment of angina pectoris and systemic hypertension 1. Nifedipine is a BCS class II drug with elimination half-life of about 2-4hrs. It shows 45-56% of oral bioavailability because of hepatic first pass metabolism. Rate limiting step in absorption of Nifedipine from gastrointestinal tract ABSTRACT The objective of the research work is to enhance the solubility and dissolution rate of Nifedipine by converting them into suitable solid lipid nanoparticles (SLNs). The method used for formulating solid lipid nanoparticles (SLNs) was high pressure homogenization followed by solvent emulsification-ultrasonication. The evaluation parameters for SLNs were drug content, entrapment efficiency, particle size, solubility study, in vitro drug release, etc. Nifedipine loaded solid lipid nanoparticles (SLNs) were characterized for drug content, entrapment efficiency, particle size, solubility study and in vitro drug release. Nifedipine loaded SLNs was prepared by using stearic acid and glycerylmonostearate as lipid and Tween 80 as stabilizer. The optimized batch (F4) contained 500mg of Glycerylmonostearate and 300mg of stabilizer. Batch F4 exhibited drug content of 88.75±0.510%, %EE of 79.31±0.119%, Particle size of 146±31.2nm, Practical yield of 91±1.21%, Solubility of 0.011mg/ml and % drug release of 71.17% at 180mins. It was concluded that the solid lipid nanoparticles (SLNs) developed by this method showed increase in solubility and dissolution rate of Nifedipine.
Pharmacology & Pharmacy, 2014
In this study, a new formulation of silica nanocomposite containing nifedipine (NI) loaded freezedried solid-lipid nanoparticles (NI-SLNs) and silica have been developed with improved flowability of powders, which can lead to the formulation of a widely acceptable oral dosage form. The stable NI-SLNs were prepared using two phospholipids, hydrogenated soybean phosphatidylcholine and dipalmitoylphosphatidylglycerol mixed with 2.5% w/v trehalose as a cryoprotectant followed by lyophilization. We employed various grades of two types of silica, such as fumed and precipitated. Silica improved the poor flow property of NI-SLNs to good category as per USP-29. In addition, most of the silica nanocomposites showed the satisfactory results in their physicochemical properties such as particle size, polydispersity index, zeta potential, and recovered potency by around 100 nm, 0.3, −50 mV, and 80%, respectively. Furthermore, it was found that NI-SLNs were easily released form nanocomposites within 30 min, therefore, suggesting an improvement of drug dissolutions. Among them, precipitated silica cooperated fairly in improving the powder characteristics as well as the physicochemical, morphological, and pharmaceutical properties.
Investigation of Variables Related to the Formulation of Apixaban Nanostructured Lipid Carriers
International Research Journal Of Pharmacy, 2018
The objective of this research was to investigate and optimize the potential of nanostructured lipid carriers (NLCs) as a carrier system for Apixaban, which is an inhibitor of coagulation factor Xa have poor solubility and low bioavailability (F=50). Nanostructured lipid carriers (NLC) of apixaban were prepared by the ultra-sonication method with the aim of improving the pharmacokinetic behavior of apixaban and to increase patient compliance. Ten formulas of NLCs were prepared using glyceryl monostearate as solid lipid, and oleic acid as liquid lipid at different ratios in addition to different surfactants include Tween 80, Tween 20, or Poloxamer188 at different ratios. The prepared formulas were characterized regarding drug content, particle size analysis, polydispersity, entrapment efficiency, Zeta-potential, FT-IR, DSC, and in vitro dissolution study. All NLC had shown entrapment efficiency within a range of 64.53 to 89.02%. All prepared NLC has a particle size in nanometer but only four formulas particle size lower than 100nm. Both entrapment efficiency and release rate were affected by lipid concentration. Formula F6 which composed of Glyceryl mono-stearate 56.83%, Oleic acid 16.5%, Tween (80) 8.88%, and water up to 100%w/w was considered as a selected formula depending on its smallest particle size (42.1nm) and good physical properties in addition to promising release profile. The optimized formulation did not show remarkable physicochemical changes during preparation according to FT-IR and DSC results. It was concluded that the formulated NLC has a potential approach for controlled release of drug which may reduce the dose frequency and improves patient compliance.
Nanotechnology Reviews
The lipid-based colloidal carriers, such as nanostructured lipid carriers (NLCs), solid lipid nanoparticles (SLNs), nanocapsules, liposomes, and microemulsion, are the latest and significant entrants in the development of drug delivery systems owing to their myriad advantages. The NLCs are second-generation SLNs having unstructured matrix, have high drug loading, and provide long-term drug stability in comparison to SLNs and other colloidal systems, which show lower drug loading and experience burst release/drug expulsion during storage. This review is aimed to summarize the formulation development and optimization strategies for NLCs as reported in the literature collected from authentic databases. Various types of NLCs, formulation components, methods of preparation, characterization parameters, optimization (statistical designs) strategies, toxicity, regulatory aspects, and their applications in oral, parenteral, ocular, pulmonary, nose-to-brain, tumor targeting, and transdermal ...
Oral drug delivery has always been considered the preferred route of drug administration. Nano-formulations are now constantly being researched for better absorption, higher bioavailability and greater therapeutic efficacy. Lipid based nanoformulations have found much favour with the formulation scientist due to their relatively higher safety profile and enhancement of bioavailability. These delivery systems are also able to protect the bioactives or drugs from the vagaries of the gastrointestinal tract. They also aid in the absorption of hydrophobic drugs which are entrapped in lipid matrices. Lipid excipients have been known to reduce efflux which is P-glycoprotein mediated and also to increase the bioavailability of bioactives which are given through the oral route.
Formulation of lipid bearing pellets as a delivery system for poorly soluble drugs
The aim of this study was to develop and characterize phospholipid bearing pellets for a poorly watersoluble drug, nisoldipine. Pellets were prepared using extrusion-spheronization technique containing microcrystalline cellulose, soy phosphatidylcholine (SPC), granulating fluid and lactose. Operational parameters such as extrusion speed, spheronization speed and residence time were evaluated. Optimal extrusion speed was found to be 50 rpm with a spheronization speed of 60 Hz and residence time of 2 min. Pellets were characterized for their size, shape, density, flow properties, friability, moisture content, surface morphology and thermal properties. Pellets were evaluated for their assay and in vitro drug release. Mathematical modeling was used to determine the release patterns of the pellets. Pellets were found to be spherical, 600-850 m size with <0.01% friability and had >70% yield. Scanning electron microscopic (SEM) studies showed a smoother external surface and a porous internal matrix. SPC incorporated pellets resulted in improved dissolution of the drug. Pellets with SPC (20 and 30%) released >90% of the drug within 24 h. The dissolution profiles of the pellets were best fitted to Korsmeyer-Peppas kinetic model. In this study, we could successfully incorporate a lipid and a water-insoluble drug into a pellet formulation with improved dissolution profile.
Lipid Nanoformulations for Oral Delivery of Bioactives: An Overview
Current Drug Therapy, 2014
Oral drug delivery has always been considered the preferred route of drug administration. Nano-formulations are now constantly being researched for better absorption, higher bioavailability and greater therapeutic efficacy. Lipid based nanoformulations have found much favour with the formulation scientist due to their relatively higher safety profile and enhancement of bioavailability. These delivery systems are also able to protect the bioactives or drugs from the vagaries of the gastrointestinal tract. They also aid in the absorption of hydrophobic drugs which are entrapped in lipid matrices. Lipid excipients have been known to reduce efflux which is P-glycoprotein mediated and also to increase the bioavailability of bioactives which are given through the oral route. In the last 20 years, about a thousand articles and reviews about oral lipid carriers have been reported. Many dosage forms have been made by modifying liposome, sometimes to overcome a disadvantage and at other times to modify the dosage form in such a manner so as to suit the requirement of the drug molecules. Various other lipidic drug delivery systems also exist which are not vesicular but being made of lipids, are equally useful for delivering lipophilic drugs. Although a Lipid Formulation Classification System exists, but there is no exhaustive review which discusses the entire lipid based, oral nanoformulations. The present review envisages discussing the various types of oral, lipid, nanosized, delivery systems available, so that an insight is gained into all these carriers, and the formulation scientist can make a judicious decision regarding choice of a lipid based carrier.