Preparation, Characterization and Stability Studies of Solid Self Emulsifying Drug Delivery System of Nifedipine (original) (raw)
Related papers
2013
The present work was aimed at improving dissolution rate of poorly soluble drug nifedipine by developing and characterizing self-micro emulsifying delivery systems (SMEDDS). The solid SMEDDS were then prepared for filling into hard gelatin capsules. Solubility of nifedipine was carried out in various oils, surfactants and co surfactants/co solvents. Twelve self emulsifying formulations were prepared using various proportions of oil, surfactants and co surfactants/co solvents in which solubility of nifedipine was high. The stability studies after introduction of nifedipine into different combinations provided the nifedipine liquid SMEDDS which were then evaluated for droplet size and percentage transmittance. The optimized liquid SMEDDS comprised of captex 100, labrasol, tween 60 and propylene glycol. Liquid SMEDDS was then converted into free flowing powder by adsorbing onto Magnesium Aluminium Silicate. Solid SMEDDS were then characterized by scanning electron microscopy (SEM) and ...
Enhancement of Solubility and Dissolution Rate of Poorly Soluble Drug Nifedipine by Solid Sedds
International Journal of Drug Delivery Technology, 2020
Nifedipine is a dihydropyridine calci channel blocking agent belongs to biopharmaceutical classification system (BCS) class-II mainly applied in the treatment of hypertension and angina-pectoris. The objective of this work is to improve the solubility and dissolution rate of nifedipine by formulating into a solid-self micro emulsifying drug delivery system (solid smedds). Methods: Oil, Surfactant, and cosurfactant were selected by solubility screening study. For the determination of the best emulsion region, a pseudo ternary diagram was prepared. Based on solubility castor oil, tween 80 and polyethylene glycol (PEG) 400 was selected in which SCOSmix (a mixture of surfactant and cosurfactant) was 1:1. Thermodynamic stability study was performed for the determination of stable smedds formulation. These formulations were evaluated for self emulsification time, drug content analysis, robustness to dilution test, particle size analysis, and in vitro diffusion study. The optimized formula...
Spontaneous Emulsification of Nifedipine-Loaded Self-Nanoemulsifying Drug Delivery System
AAPS PharmSciTech, 2014
Self-nanoemulsifying drug delivery system (SNEDDS) can be used to improve dissolution of poorly water-soluble drugs. The objective of this study was to prepare SNEDDS by using ternary phase diagram and investigate their spontaneous emulsifying property, dissolution of nifedipine (NDP), as well as the pharmacokinetic profile of selected SNEDDS formulation. The results showed that the composition of the SNEDDS was a great importance for the spontaneous emulsification. Based on ternary phase diagram, the region giving the SNEDDS with emulsion droplet size of less than 300 nm after diluting in aqueous medium was selected for further formulation. The small-angle X-ray scattering curves showed no sharp peak after dilution at different percentages of water, suggesting non-ordered structure. The system was found to be robust in different dilution volumes; the droplet size was in nanometer range. In vitro dissolution study showed remarkable increase in dissolution of NDP from SNEDDS formulations compared with NDP powders. The pharmacokinetic study of selected SNEDDS formulation in male Wistar rats revealed the improved maximum concentration and area under the curve. Our results proposed that the developed SNEDDS formations could be promising to improve the dissolution and oral bioavailability of NDP.
AAPS PharmSciTech, 2014
A simple but novel mixed surfactant system was designed to fabricate a self-nanoemulsifying drug delivery system (SNEDDS) based on hydrophilic-lipophilic balance (HLB) value. The impacts of HLB and molecular structure of surfactants on the formation of SNEDDS were investigated. After screening various oils and surfactants, nifedipine (NDP)-loaded liquid SNEDDS was formulated with Imwitor ® 742 as oil and Tween ® /Span ® or Cremophor ® /Span ® as mixed surfactant. Droplet size of the emulsions obtained after dispersing SNEDDS containing Tween ® /Span ® in aqueous medium was independent of the HLB of a mixed surfactant. The use of the Cremophor ® /Span ® blend gave nanosized emulsion at higher HLB. The structure of the surfactant was found to influence the emulsion droplet size. Solid SNEDDS was then prepared by adsorbing NDP-loaded liquid SNEDDS comprising Cremophor ® RH40/Span ® 80 onto Aerosil ® 200 or Aerosil ® R972 as inert solid carrier. Solid SNEDDS formulations using higher amounts (30-50% w/w) of Aerosil ® 200 exhibited good flow properties with smooth surface and preserved the self-emulsifying properties of liquid SNEDDS. Differential scanning calorimetry and X-ray diffraction studies of solid SNEDDS revealed the transformation of the crystalline structure of NDP due to its molecular dispersion state. In vitro dissolution study demonstrated higher dissolution of NDP from solid SNEDDS compared with NDP powder.
Brazilian Journal of Pharmaceutical Sciences
In order to develop a self-nanoemulsifying system, three components, olive oil, Tween 80, and Capmul, were used to construct a ternary phase diagram that helped to find the optimum formulation, which was loaded with nifedipine. The effect of sonication on drug loading was also evaluated. After that, measurement of the droplet size, size distribution, zeta potential, and scanning electron microscopy were conducted for evaluation and characterisation of the formulations. The phase diagram of four formulations showed nanosizes below 200 nm; however, only one was selected to be loaded with nifedipine. The selected formulation had the lowest droplet size of 98 nm and size distribution 0.192, and was composed of 48% Tween 80, 32% Capmul, and 20% olive oil. The nifedipine self-nanoemulsifying drug delivery system (SNEDDS) showed a significant change in the particle size (97 nm) and size distribution (0.257) after sonication. Its zeta potential was-32.3 mV indicating good stability. The SEM photographs of nifedipine showed particles with spherical shape and smooth surface. Finally, a self-nanoemulsifying formulation containing nifedipine, loaded in olive oil, was successfully prepared by mixing the oil with various types of surfactants and co-surfactants. A significant nifedipine self-nanoemulsifying system was developed and significantly improved accordingly.
Review of formulation and evaluation of self-micro emulsifying drug delivery system (SMEDDS)
ScienceRise: Pharmaceutical Science
Approximately half of the new drug applicants that reach formulation have poor water solubility. Oral delivery has been the main route of drug administration for the chronic treatment of numerous diseases. In different cases, in oral conveyance, 50 % of the medication compound is hampered because of the high lipid soluble or fat soluble of the medication itself. Around 40 % of new drug applicants show low solubility in water, which prompts poor oral bioavailability, high Intra and Intersubject changeability, and deficiency of dose proportionality Aim of review. The main aim of this review article is to gather the information related to design and evaluation of SMEDDS. These information can be utilized to enhance the bioavailability of the poorly aqueous soluble drug for various types of orally administered drugs. In this review article, various literature are reviewed and summerised in single paper to serve as reference guide to various research scholars and researchers working on self-micro-emulsifying drug delivery systems. Materials and Methods. To prepare this manuscript various keywords were searched in different search engine such as Google, Yahoo and Bing etc. This review article reviews the recent work done in the field of SMEDDS. It comprises review of literatures available in public domain and formulation of SMEDDS and its characterization is summarized in this article. Result. The various strategies to developed poor aqueous soluble drug for improvement of bioavailability for example, salt development and molecular size reduction of the compound might be one technique to enhance the dissolution rate of the drug. In any case, these methods have their limitations. SMEDDS is one of the novel applications for the delivery of low water soluble and low bioavailability of drug. SMEDDS is a method to improve the aqueous solubility of the medication; SMEDDS are described as isotropic blenders of oils, surfactants, and co-surfactant. Upon slightly stir followed by dilution with distilled water, for example, gastrointestinal liquids, these techniques can define clear o/w micro emulsion. SMEDDS is first choice and key technology for developing the lipophilic drug and other different factors that chance to affect the oral bioavailability. Conclusions. This review paper attempts to describe the preparation of SMEDDS and furthermore discusses the development of pseudo ternary phase diagram for SMEDDS. It describes the mechanism and method of preparation involved in SMEDDS. The capability of oral absorption of drug compound from the SMEDDS relies upon numerous formulation−related parameters, for example, surfactant concentration, oil/surfactant ratio, and hydrophobicity of emulsion, globule size and charge, in vitro, in vivo all of which basically characterized the ability of self-emulsification. SMEDDS are administered as unit dosage form and it also protect the degradation of drug.
2016
Poorly water soluble drug candidates are becoming more prevalent and it has been estimated that 40-50% of drug molecules are poorly soluble in aqueous media or have a low permeability which does not allow for their adequate absorption from gastrointestinal tract following by oral administration. Formulation scientists have to adopt different strategies to enhance their absorption. Lipidic formulations are seen to be a promising approach to combat the challenges and especially self-microemulsifying drug delivery(SMEDDS) system approach are used to increase the absorption of poorly absorbed drug which ultimately increased there bioavailability. The attempts of various scientist to convert the liquid SMEDDS to solid-SMEDDS by adsorption, spray drying, lyophilisation, melt granulation and extrusion techniques. Formulation of SMEDDS is a potential strategy to deliver poorly soluble drug and low absorption drug with enhanced dissolution rate and bioavailability.
Journal of Pharmaceutical Research
As the development of modern drug discovery techniques, there has been increase in the number of pharmaceutical compounds that are poorly water soluble. These lipophilic compounds possess low dissolution rate and therefore low bioavailability. The Formulation scientists should adopt various strategies to enhance their absorption. This paper is an insight for improving the solubility of poorly water soluble compounds. Lipidic formulations are found to be a promising approach to combat the solubility challenges. Self MicroEmulsifying Drug Delivery Systems (SMEDDS) are gaining more attention for improving the solubility of the lipophilic drugs. SMEDDS are isotropic mixtures of oil, surfactant and co surfactant and are vital tool in solving low bioavailability problems of poorly soluble drugs. Lipophilic drugs can be dissolved in these systems, enabling them to be administered per orally. When this is released into the lumen it results in w/o microemulsion with the aid of G.I fluid. This present review describes various formulation components, mechanism of emulsification, biopharm aspects, characterization methods and application of SMEDDS.
Self Emulsifying Drug Delivery System: A Tool in Solubility Enhancement of Poorly Soluble Drugs
2012
Low aqueous solubility and thereby low oral bioavailability is a major concern for formulation scientist as many recent drugs are lipophillic in nature and their lower solubility and dissolution is a major drawback for their successful formulation into oral dosage forms. Aqueous solubility of drugs can be increased by different methods such as salt formation, solid dispersion, complex formation but Self Emulsifying Drug Delivery System (SEDDS) is gaining more attention for improving the solubility of lipophillic drugs. SEDDS are ideally isotropic mixtures of drug, oil, surfactant and/or co surfactant. They spontaneously form emulsion on mixing with water with little or no energy input. Generally SEDDS are prepared using triglycerides and non ionic surfactants. The present review provides an updated account of the advancements in SEDDS with regard to the selection of lipid systems for current formulations, dosage forms for SEDDS, solidification techniques, characterization and their ...
Design and Evaluation of Self-Emulsifying Drug Delivery Systems (SEDDS) of Nimodipine
The ability of self-emulsifying drug delivery systems (SEDDS) to improve solubility, dissolution rate and bioavailability of a poorly water-soluble calcium channel blocker, nimodipine (NM) was evaluated in the present investigation. Solubility of NM in various oils, surfactants and cosurfactants was determined. The influence of the ratio of oil to surfactant + cosurfactant, pH of aqueous phase on mean globule size of resulting emulsions was studied by means of photon correlation spectroscopy. The NM loaded SEDDS selected for the in vitro and in vivo studies exhibited globule size less than 180 nm. In vitro dissolution studies indicated that NM loaded SEDDS could release complete amount of NM irrespective of the pH of the dissolution media. Pharmacokinetics of NM suspension, NM oily solution, NM micellar solution and NM SEDDS were evaluated and compared in rabbits. Relative bioavailability of NM in SEDDS was significantly higher than all the other formulations. NM loaded SEDDS were subjected to various conditions of storage as per ICH guidelines for 3 months. NM SEDDS successfully withstood the stability testing.