Development, Characterization, and Pharmacodynamic Evaluation of Hydrochlorothiazide Loaded Self-Nanoemulsifying Drug Delivery Systems (original) (raw)
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International Journal of Pharmaceutical Investigation, 2018
Delivering drugs via oral route represents the most widely and convenient route being the easiest in administration, the most compliant for the patient, in addition to, the possibility to design many dosage forms. Moreover, it is the most economical, especially that, it is characterized by the least sterility constraints. However, the major challenge with the formulation of oral dosage forms lies with their poor oral bioavailability. Various factors such as poor aqueous solubility, lower drug permeability, Objective: The present study was aimed at formulating and evaluating a novel solid self-nano emulsifying drug delivery system (SNEDDS) to increase the solubility and bioavailability of hydrochlorothiazide (HCZ). Enhancing both solubility and bioavailability of drugs remain the cornerstone for achieving successful outcomes of delivery systems. Furthermore, employing nanotechnology-based formulations such as SNEDDS offers important advantage; the most important is the protection of the drug from enzymatic or chemical degradation. Materials and Methods: Liquid SNEDDS (L-SNEDDS) was prepared by adding a drug to oil, surfactant, and co-surfactant and heated up to at 60°C under continuous stirring. Solid SNEDDS (S-SNEDDS) was prepared by mixing L-SNEDDS with microcrystalline cellulose in 1:1 proportion. Results: The scanning electron microscopy showed that S-SNEDDS was spherical with an average particle size of 66.9 nm and 69.2 nm for both L-SNEDDS and S-SNEDDS, respectively. Ex vivo skin permeation study indicated that 100% drug was released from both the L-SNEDDS and S-SNEDDS formulation SF3 in 3 h. Analysis of variance test showed significant differences (Moderately significant P < 0.01) in the values when compared to a marketed product. Conclusion: The prepared S-SNEDDS helped in improving the solubility of the poorly soluble HCZ, which is a step forward toward bioavailability enhancement and thus increased therapeutic efficacy of the drug.
FORMULATION AND EVALUATION OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEMS
It has become clear that self-nanoemulsifying drug delivery systems (SNEDDS) are a potential method for improving the solubility and bioavailability of medicines that are not highly watersoluble. Using Capmul MCM, Tween 80, Transcutol P, and olmesartan medoxomil as the oil, surfactant, co-surfactant, and medication, respectively, an optimal SNEDDS formulation was created in this work. The improved formulation's physicochemical characteristics, in vitro drug release profile, pharmacokinetic parameters, and acute and sub chronic toxicity were assessed. The findings revealed that the SNEDDS formulation had a high drug content of 95%, a zeta potential of-20 mV, and a particle size of 50 nm. The medication released consistently throughout a 12-hour period, according to the in vitro drug release profile. The pharmacokinetic analysis demonstrated that, in comparison to the pure medication, the SNEDDS formulation had a larger Cmax, AUC, and longer elimination half-life. According to tests on acute and subchronic toxicity, the formulation was well tolerated at low dosages while harmful effects were dose-dependent at higher concentrations. Overall, the findings showed that SNEDDS might be used as a drug delivery system to enhance the solubility, bioavailability, and pharmacokinetic characteristics of medicines that are poorly water-soluble.
Developments in recent drug discovery programs, yields a large proportion of novel pharmacologically active molecules that are lipophilic and poorly soluble ,which is a major challenge for pharmaceutical researchers to enhance the oral bioavailability of such drug molecules. Compared to conventional oral dosage forms, Self nanoemulsifying drug delivery systems (SNEDDS) possesses potential advantages like ease of manufacture and scale up, quick onset of action, reduction in drug dose, reduction in inter and intra subject variability and food effects and minimize problems associated with filling of liquid SNEDDS in capsules. Several recent works on Self nanoemulsifying drug delivery systems suggests the commercial suitability of the system in improving the solubility and bioavailability of such drugs. The physicochemical properties, drug solubilization capacity and physiological fate considerably helps in the selection of the SNEDD components. The composition of the SNEDDS can be optimized mainly with the help of phase diagrams, whereas statistical experimental design can be used for further optimization. The transition of liquid SNEDDS to solid SNEDDS has also been accomplished by researchers. Solid-self nanoemulsifying drug delivery system focus on the incorporation of liquid/semisolid self nano emulsifying ingredient into solids by different solidification techniques like adsorption to solid carrier, spray drying, melt extrusion, nanoparticle technology and melt granulation. The present article gives more specification on spontaneous/rapid forming nanoemulsions or self nanoemulsifying systems for oral drug delivery by adsorption technique and gives complete information about formulation, method of preparation, characterization and application in solid dosage form of self nanoemulsifying drug delivery system.
Review Article Self Emulsifying Drug Delivery System: A Review
2013
The oral route is the favourite route for chronic drug therapy, majority of drugs are frequently administered through oral route. Oral drug delivery systems being the most cost-effective to manufacture, have always lead the worldwide drug delivery market. This oral route may be a problem route for drug molecules which exhibit poor aqueous solubility. When a drug is administered by oral route the first step for it to get absorbed is its solubilisation followed by permeation. However, an increasing number of poorly soluble drug candidates with low, variable and food-dependent bioavailability are facing the pharmaceutical industry today. Approximately 40% of new chemical entities exhibit poor aqueous solubility and present a major challenge to modern drug delivery system. A rate limiting step for the absorption of these drugs is often their solubilisation in the gastrointestinal tract. These drugs are classified as class II drug by Biopharmaceutical classification system (BCS), drugs with poor aqueous solubility and high permeability. Thus for such drug substances to be effectively absorbed, there is a need to increase their dissolution rate. Oral delivery of such drugs is complicated for the reason that of their low bioavailability, high intra-and inter-subject variability, and not have dose linearity. To overcome these problems, a variety of strategies have been developed including the use of surfactants, lipids, permeation enhancers, micronization, salt formation, cyclodextrins, nanoparticles and solid dispersions, and self emulsifying drug delivery system.
Drug discoveries & therapeutics, 2010
This study sought to formulate and evaluate a self-nanoemulsified drug delivery system (SNEDDS) for clotrimazole (CT), a poorly water-soluble antimycotic drug, used in vaginal delivery. SNEDDS was developed to increase the CT dissolution rate, solubility, and ultimately bioavailability. The solubility of CT in various oils, surfactants, and co-surfactants was determined. Based on solubility studies, oil phase (oleic acid without or with coconut oil), surfactant (Tween 20), and co-surfactants (PEG 200 and n-butanol) were selected and grouped in two combinations for phase studies. Pseudo-ternary phase diagrams were used to evaluate the area of self-nanoemulsification. Essential properties of the prepared systems with regard to emulsion droplet size and turbidity value were determined. In order to investigate the potential for interaction between any of the SNEDDS ingredients used, FTIR spectroscopy was performed. In vitro release studies were performed with SNEDDS formulations in caps...
2021
Self nano emulsifying drug delivery systems (SNEDDs) gained much attention in the last decades since, such systems considered one of the most favorable and efficient approaches to enhance solubility, increase drug absorption and hence, enhance its oral bioavailability of poorly water soluble (lipophilic) drug moieties. Owing to their unique properties and advantages over the other conventional dosage forms, many literatures investigate the change physicochemical properties, pharmacokinetic and pharmacodynamics of self emulsifying formulation compared to both pure drug and its conventional dosage form and always reported significant improvement using SNEDDs. This review discus the composition, advantages and mechanism of action of liquid SNEDDs and some techniques used for solidification of liquid formulations to overcome its drawbacks.
2017
Developments in recent drug discovery programs, yields a large proportion of novel pharmacologically active molecules that are lipophilic and poorly soluble ,which is a major challenge for pharmaceutical researchers to enhance the oral bioavailability of such drug molecules. Compared to conventional oral dosage forms, Self nanoemulsifying drug delivery systems (SNEDDS) possesses potential advantages like ease of manufacture and scale up, quick onset of action, reduction in drug dose, reduction in inter and intra subject variability and food effects and minimize problems associated with filling of liquid SNEDDS in capsules. Several recent works on Self nanoemulsifying drug delivery systems suggests the commercial suitability of the system in improving the solubility and bioavailability of such drugs. The physicochemical properties, drug solubilization capacity and physiological fate considerably helps in the selection of the SNEDD components. The composition of the SNEDDS can be optimized mainly with the help of phase diagrams, whereas statistical experimental design can be used for further optimization. The transition of liquid SNEDDS to solid SNEDDS has also been accomplished by researchers. Solidself nanoemulsifying drug delivery system focus on the incorporation of liquid/semisolid self nano emulsifying ingredient into solids by different solidification techniques like adsorption to solid carrier, spray drying, melt extrusion, nanoparticle technology and melt granulation. The present article gives more specification on spontaneous/rapid forming nanoemulsions or self nanoemulsifying systems for oral drug delivery by adsorption technique and gives complete information about formulation, method of preparation, characterization and application in solid dosage form of self nanoemulsifying drug delivery system.
Pharmaceutical Sciences Asia, 2020
Nanotechnology is strongly accepted as the crucial approach in drug delivery that can influence the therapeutic performance of hydrophobic drugs. Self-nanoemulsifying drug delivery systems (SNEDDS) are one of the proven methods that can increase solubility and bioavailability of poorly water soluble drugs. SNEDDS are anhydrous homogenous liquid mixtures consisting of oil, surfactant, co-surfactant, and drugs, which spontaneously form o/w nanoemulsions when diluted with water under gentle agitation. SNEDDS provide several potential effects on oral drug delivery. This article presents an overview of SNEDDS along with their basics; such as, composition, preparation, characterization, potential effects associated with oral delivery, applications, commercially available products, advanced technology associated with SNEDDS, and trending.
Design and evaluation of self-nanoemulsifying drug delivery systems(SNEDDS) for Gliclazide
Der Pharmacia Lettre, 2010
Self-nanoemulsifying drug delivery systems (SNEDDS) were developed with the objective to overcome problems associated with the delivery of Gliclazide, a poorly bioavailable, anti-diabetic having pH dependant solubility. Solubility of Gliclazide in oily phases and surfactants were determined to identify components of SNEDDS. Various surfactants and co-surfactants were screened for their ability to emulsify selected oily phases. Ternary phase diagrams were constructed to identify area of nanoemulsification for the selected systems. The influence of Gliclazide and pH of dilution medium on the phase behavior of selected system were assessed. The globule size of optimized Gliclazide SNEDDS in various dissolution media was determined to check the effect of pH on its behavior. The optimized Gliclazide SNEDDS needed surfactant content less than 55% and yielded nanoemulsion of mean globule size 146 nm, which was not affected by the pH of dilution medium. The optimized SNEDDS released the Gliclazide drug completely within 20 min irrespective of the pH of dissolution medium.