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During the last decades, much attention has been focused on SNEDDS approach to resolve concerns of BCS II class drugs with accentuation on upgrading the solubility and bioavailability. The present hypothesis confirms the theory that SNEDDS can reduce the impact of food on Candesartan solubilization, thereby offering the potential for improved oral...
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Citations
... All the responses were fitted in the least fit squares regression analysis using JMP 16 (Trial). Various outcomes of the mathematical model, like the actual vs predicted plot, ANOVA analysis, parameter estimates, model equation, prediction profiler, response surface, contour profilers, Pareto charts and optimization desirability, were determined to validate the model [13]. The desirability function was used for the selected responses for the optimization process. ...
Background
The present study focused on developing a superior adsorbent carrier (microparticles) to solidify the self-emulsifying drug delivery system. The two approaches, solvent evaporation and spray drying, were explored to synthesize the microparticles using chitosan (CH) and EDTA disodium. The 3 ² full factorial design was applied to optimize the microparticle process produced by both methods.
Results
The various characterization evaluations of the microparticles revealed amide linkages between the CH and EDTA disodium, and XRD results showed that microparticles were amorphous. The SE-CHEM (C 2 ) and SD-CHEM (Y 1 ) optimized microparticles were free-flowing and had percentage yield (%), 96 ± 1.2 and 58 ± 1.1, zeta potential (mV), 9 ± 0.44 and 4 ± 0.13, and particle size (μm), 3 ± 0.57 and 2 ± 0.4, respectively. SEM images showed uneven surfaces with wide void spaces and flaky texture for optimized microparticles Y 1 and C 2 , respectively. The SE-CHEM (C 2 ) had an oil adsorption capacity (OAC %) of 46 ± 0.54 and 60 ± 0.77, and oil desorption capacity (ODC %), 38 ± 0.65 and 56 ± 0.86, for Labrafac and Cremophor RH 40, respectively. The SD-CHEM (Y 1 ) had an oil adsorption capacity (OAC %) of 59 ± 0.71 and 68 ± 0.39, and oil desorption capacity (ODC %), 54 ± 0.11 and 65 ± 0.74, for Labrafac and Cremophor RH 40, respectively. In the surface free energy components analysis, the SE-CHEM (C 2 ) had an enhanced dispersive component [ γ LW (mJ/m ² )] of 32 ± 0.68 and 37 ± 0.47 for Labrafac and Cremophor RH 40, respectively. The SD-CHEM (Y 1 ) had an enhanced dispersive component [ γ LW (mJ/m ² )] of 48 ± 0.7 and 52 ± 0.41 for Labrafac and Cremophor RH 40, respectively. The SE-CHEM (C 2 ) had enhanced dynamic advancing contact angles [ θ a (°)] of 75 ± 0.19 and 78 ± 0.75 for Labrafac and Cremophor RH 40, respectively. The SD-CHEM (Y 1 ) had enhanced dynamic advancing contact angles [ θ a (°)] of 74 ± 0.6 and 80 ± 0.21 for Labrafac and Cremophor RH 40, respectively.
Conclusion
All the findings indicate that the microparticles have superior characteristics to serve as the adsorbent base for solid self-emulsifying drug delivery systems.
... As concentration was exceeded to 70% it caused an increase in droplet size. The increase in water content can easily passes the oil droplet, were easily undergoes the "self-emulsification" process 54 ...
SNEDDS were developed with the objective of treating low bioavailability of drugs for antiviral drugs due to its low solubility. The scientist has increased their interest in improving bioavailability and absorption of poorly-water soluble drugs using Self-Emulsifying lipid technology. SNEDDS was an isocratic mixture contains an Oil, Surfactant, Co-surfactant, and Drug in accurate amount. The SNEDDS was primarily prepared as liquid-SNEDDS, but S-SNEDDS was more stable as compared to L-SNEDDS. As viral infection was major threat for people due to its limited efficacy and Serious adverse effects. The most damaging viral diseases was treated with help of SNEDDS as delivery system. They were a leading cause of morbidity and mortality. The plant and plant source were major source from which the extracted metabolites used for synthesis of drug through metabolic pathway. The phytochemicals and extracts were better and safe alternative for synthetic drugs. The phytochemicals like Curcumin, Myricetin, Apigenin etc. used as drug for treating antivirals using SNEDDS. This technique was used for quantitative and qualitative analysis. Also, the ternary phase diagram gives dramatic representation of Oil, surfactant and Co-surfactant which shows its concentration. Some characterization techniques were Droplet size, Zeta potential, XRD, DSC, FTIR, and TGA. Also, QbD provides a platform for systemic production of drug formulations. QbD was used for its better bioavailability.
... The drug was taken in a stopper glass vial of 5 mL capacity and mixed for 10 min with each component by using a vortex mixer. The vials were kept in an isothermal shaker (GFL1092, Burgwedel, Germany) at 50 ± 1.0 •C for 72 h until homogeneity is achieved [9,10]. The homogenate centrifugation was carried out at 1500 rpm for 10 minutes or 5000 rpm for 5 mints. ...
The aim of this study was to prepare an oral administrable SNEDDS for poorly water soluble drugs Bilastine. To choose the SNEDDS excipients, a ternary phase diagram and solubility assessment were conducted. A components of oil (capmul PG-NF) surfactant (Tween 40) and co-surfactant (Capryol 90) were used as the excipients. The optimized formulation was characterized for In-vitro analysis. The prepared S-SNEDDs exhibited good flow characteristics and Particle size (148.5dnm), zeta potential (−28.6), PDI (0.242), drug loading efficiency, % CDR of the optimized S-SNEDDs [TP3PG1 (2:8)] was found to be 103.61 ±0.678, 98.65% respectively. The formulation was stable over a 3-month storage period at 25 ◦C and 4 ◦C in terms of particle size, physical appearance, and drug loading. Overall, a range of lipid based SNEDDS liquid, solid formulations were successfully developed and seem to be a promising alternative to improving the solubility of poorly water-soluble drugs and evaluating In-vitro characterizations.
... The formulated Cr-NLCs dispersion was evaluated for stability studies for 90 days at 4 °C and 25 °C. After 90 days, preparations were assessed for p-size, PdI, % entrapment efficiency and zeta potential (ζ) in triplicate [53]. ...
Background
The goal of current research work is to develop and optimize curcumin-encapsulated nanostructured lipid carriers and to enhance therapeutic effect of curcumin after oral administration.
Method
Curcumin-loaded nanostructured lipid carriers were developed by a single-step one-pot microwave-assisted technique. The preparation of curcumin-loaded nanostructured lipid carriers was optimized by employing two factors and three levels central composite design (Design Expert® software) taking concentration of lipid blend and surfactant as independent variables and particle size, polydispersity index, and zeta potential as dependent variables, to investigate the effect of formulation ingredients on the physicochemical characteristics of nanostructured lipid carriers. The optimized batch was investigated by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, high-resolution transmission electron microscopy, in vitro drug release, stability studies, cytotoxicity, and in vivo anthelmintic studies.
Results
The average particle size, polydispersity index, and zeta potential of the optimized batch were found to be 144 nm, 0.301, and − 33.2 mV, respectively, with an entrapment efficiency of 92.48%. The results of high-resolution transmission electron microscopy confirmed spherical shape of particles. In vivo antiparasitic studies included determining the duration of paralysis and eventual death of earthworms in the presence of test samples. The results of in vivo studies showed good anthelmintic potential for curcumin-loaded nanostructured lipid carriers as compared to albendazole in different concentrations. Cytotoxicity studies also confirmed the formulation to be nontoxic to Vero cells. In vitro drug release study showed 90.76 ± 0.01% release of curcumin in 24 h by following the Korsmeyer-Peppas model of release kinetics.
Conclusion
The aforementioned results imply that microwave-developed nanostructured lipid carriers could be promising drug carriers and will aid in their fabrication for oral administration as a possible alternative for the treatment of other parasitic infections.
Graphical Abstract
... 17 Verma et al also improved the rate of dissolution and oral bioavailability of poorly soluble candesartan by formulating it into SNEDDS. [18][19][20][21] Accordingly, the aim of the current study is to develop an MCA-loaded SNEDDS formulation to achieve improvement of pharmacokinetic behavior. The selected formulation was evaluated by in vitro dissolution and in vivo studies. ...
... High drug solubilization is important for improving the efficiency of drug loading into carriers with concomitant advances in oral bioavailability. 18 Hence, the selection of media to formulate SNEDDS is critical. The solubility of MCA in diverse oil phases, surfactants, and co-surfactants has been evaluated ( Figure 2). ...
Purpose
Madecassic acid (MCA) is a natural triterpenoid isolated from centellae herba that has diverse biological effects, such as anti-inflammatory, antioxidant, and anticancer activities. However, the efficacy of MCA is limited by low oral bioavailability caused by its extremely poor aqueous solubility. This study aimed to develop a self-nanoemulsifying drug delivery system (SNEDDS) for MCA to improve its oral absorption.
Methods
The utilized oil phases, surfactants, and co-surfactants for SNEDDS were selected based on the solubility of MCA and emulsification efficiency. The optimized formulation was characterized for pharmaceutical properties and its pharmacokinetic behavior was examined in rats. Besides, the intestinal absorption property of MCA was investigated using in situ single-pass intestinal perfusion and intestinal lymphatic transport.
Results
The optimized nanoemulsion formula consists of Capryol 90:Labrasol:Kolliphor ELP:Transcutol HP in a weight ratio of 1:2.7:2.7:3.6 (w/w/w/w). MCA-loaded SNEDDS presented a small droplet size (21.52 ± 0.23 nm), with a zeta potential value of −3.05 ± 0.3 mV. Compared with pure MCA, SNEDDS had a higher effective permeability coefficient and showed 8.47-fold and 4.01-fold of maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC), respectively. Cycloheximide was pretreated before the experiment to evaluate the degree of lymphatic uptake. The results showed that cycloheximide greatly influenced the absorption of SNEDDS, resulting in 82.26% and 76.98% reduction in Cmax and AUC, respectively.
Conclusion
This study reports the MCA-loaded SNEDDS with distinctly enhanced in vitro and in vivo performance compared with pure MCA and concludes that the SNEDDS formulation could be a viable and effective strategy for improving the dissolution rate and bioavailability of poor aqueous-soluble ingredients.
... Centrifugation of the developed formulations was carried out at 4000 g for 5 min and phase separation was checked. 25 The test was considered passed when there was no phase separation and vice versa. ...
... Emulsion becomes cloudy by heating, and the temperature at which cloudiness is observed is called the cloud point. 25 For determination of the cloud point, an aliquot (1 mL) of each formulation was diluted with purified water (200 mL) and heated on a water bath. The temperature was gradually raised, and the point at which cloudiness was observed was recorded. ...
Background
Self-emulsifying drug-delivery systems (SEDDSs) are designed to improve the oral bioavailability of poorly water-soluble drugs. This study aimed at formulating and characterization of SEDDS-based tablets for simvastatin using castor and olive oils as solvents and Tween 60 as surfactant.
Methods
The liquids were adsorbed on microcrystalline cellulose, and all developed formulations were compressed using 10.5 mm shallow concave round punches.
Results
The resulting tablets were evaluated for different quality-control parameters at pre- and postcompression levels. Simvastatin showed better solubility in a mixture of oils and Tween 60 (10:1). All the developed formulations showed lower self-emulsification time (˂200 seconds) and higher cloud point (˃60°C). They were free of physical defects and had drug content within the acceptable range (98.5%–101%). The crushing strength of all formulations was in the range of 58–96 N, and the results of the friability test were within the range of USP (≤1). Disintegration time was within the official limits (NMT 15 min), and complete drug release was achieved within 30 min.
Conclusion
Using commonly available excipients and machinery, SEDDS-based tablets with better dissolution profile and bioavailability can be prepared by direct compression. These S-SEDDSs could be a better alternative to conventional tablets of simvastatin.
... Volume was made up to 2 ml with distilled water. Absorbance was taken at 412 nm [30]. ...
Background
Drugs with high first-pass metabolism or that are susceptible to enzymatic degradation can be administered through the nasal route to avoid their degradation. Lurasidone exhibits less toxicity and side effects as compared to its sister drugs like risperidone, ziprasidone, clozapine, etc.
Objectives
The present study aimed to develop Lurasidone loaded niosomes for nasal delivery.
Methods
Lurasidone niosomes were developed by adapting the ether injection method and optimized using a central composite design. In vitro and in vivo studies were conducted using optimized formulation.
Results
The findings showed that the optimized formulation exhibited a particle size of 159.02 ± 0.58 nm and an entrapment efficiency of 91.6 ± 1.6 %. The findings from the nasal histopathological analysis revealed that the optimized formulation was non-irritant and non-toxic for nasal mucosa. The findings from in vitro studies revealed 94.61 ± 0.27 % of drug release from optimized formulation F7 throughout 24 hrs. The findings of in vivo (Albino Wistar rats) studies demonstrated that various pharmacokinetic parameters (Cmax, Tmax, AUC(0-24), T1/2, Vd and Cl) and pharmcodynamic parameters (conditioned avoidance response, biochemical estimation using oxidative markers such as superoxide dismutase, malondialdehyde and glutathione) were significantly improved compared to marketed tablets (Lurasid® 40 mg) and pure drug suspension. Optimized formulation F-7 exhibited 4.9 times more bioavailability than that of pure drug suspension following intranasal administration.
Conclusion
These findings indicate that nasal niosomal formulation of Lurasidone HCl is a promising nanoplatform for enhancing the overall performance of Lurasidone. These results could open new avenues into the future of nanomedicine.
... Most treatments are associated with severe toxicity, are cost-effective, and are unacceptable for long-term use. 245,246 Nanocarrier systems introducing CDs may improve the prolongation time of drugs in systematic circulation, reduce toxicity and biocompatibility. 247 Recent progress in nanotechnology and chemistry of CDs delivers diverse designs of nano delivery systems such as micelles, liposomes, niosomes, nanocarriers, CD-drug conjugates with full host-guest interaction and non-covalent forces by using CDs. ...
Anti-cancer drugs are mostly limited in their use due to poor physicochemical and biopharmaceutical properties. Their lower solubility is the most common hurdle limiting their use upto their potential. In the recent years, the cyclodextrin (CD) complexation have emerged as existing approach to overcome the problem of poor solubility. CD-based nano-technological approaches are safe, stable and showed well in vivo tolerance and greater payload for encapsulation of hydrophobic drugs for the targeted delivery. They are generally chosen due to their ability to get self-assembled to form liposomes, nanoparticles, micelles and nano-sponges etc. This review paper describes a birds-eye view of the various CD-based nano-technological approaches applied for the delivery of anti-cancer moieties to the desired target such as CD based liposomes, niosomes, niosoponges, micelles, nanoparticles, monoclonal antibody, magnetic nanoparticles, small interfering RNA, nanorods, miscellaneous formulation of anti-cancer drugs containing CD. Moreover, the author also summarizes the various shortcomings of such a system and their way ahead.
... Nanomaterials are used for therapeutics in the healthcare sector, treatment for cancer, and diagnosis of disease. But in addition to their advantages, they also possess several undesirable effects, among which an increase in the absorption rate is the most important [17][18][19]. They increase the absorption rate as a result of the increased surface area of the nanomaterials, which allows increased absorption rate by the surrounding tissues leading to the generation of several unintended results [20]. ...
Scientists are focusing immense attention on polymeric nanocarriers as a prominent delivery vehicle for several biomedical applications including diagnosis of diseases, delivery of therapeutic agents, peptides, proteins, genes, siRNA, and vaccines due to their exciting physicochemical characteristics which circumvent degradation of unstable drugs, reduce toxic side effects through controlled release, and improve bioavailability. Polymers-based nanocarriers offer numerous benefits for in vivo
drug delivery such as biocompatibility, biodegradability, non-immunogenicity, active drug targeting via surface modification, and controlled release due to their pH—and thermosensitive characteristics. Despite their potential for medicinal use, regulatory approval has been achieved for just a few. In this review, we discuss the historical development of polymers starting from their initial design to their evolution as nanocarriers for therapeutic delivery of drugs, peptides, and genes. The review article
also expresses the applications of polymeric nanocarriers in the pharmaceutical and medical industry with a special emphasis on oral, ocular, parenteral, and topical application of drugs, peptides, and genes over the last two decades. The review further examines the practical, regulatory, and clinical considerations of the polymeric nanocarriers, their safety issues, and directinos for future research.
... Restoration of normal acetylation apoptosis cell cycle arrest may occur due to the presence of anticancer properties in HDAC inhibitor vorinostat [10]. However, vorinostat is plagued by low water solubility (0.2 mg/mL), low permeability, and poor pharmacokinetics, which results in difficulty for parenteral formulation [11,12]. Vorinostat is also plagued by suboptimal pharmacokinetics including low bioavailability (43% for humans and 11% for rats), extensive serum clearance, and a short elimination half-life of approximately 2 h in both animal and human studies [13][14][15][16][17]. ...
Background
Vorinostat is a histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) with anticancer properties. However, it is plagued by low water solubility, low permeability (BCS class IV drug), and suboptimal pharmacokinetics. The purpose of the present study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of vorinostat. Capryol 90, labrasol, and polyethylene glycol (PEG 400) were selected as oil phase, surfactant, and co-surfactant, respectively. The vorinostat self-microemulsifying drug delivery systems were tested for self-microemulsifying time, phase separation, effect of pH, droplet size, zeta potential, dilution study, Fourier-transform infrared (FT-IR) spectroscopy analysis, and field emission scanning electron microscopy (FESEM). A rat model in vivo pharmacokinetic study was conducted for the optimized formulation against vorinostat pure drug powder.
Results
The results from the characterization studies showed that the optimized formulation (F7) self-microemulsification time was 1.4 ± 0.05 min and no precipitation or phase separation was observed. The mean droplet size, polydispersity index (PDI), and zeta potential of the optimized formulation (F7) were found to be 272.9 ± 82.7 nm, 0.415, and − 57.2 mV, respectively. The pharmacokinetic parameters of the optimized formulation (F7) showed a 1.6-fold increase in maximum concentration ( C max ) and a 3.6-fold increase in area under the curve (AUC (0−∞) ), in comparison with pure drug in suspension.
Conclusions
The findings suggest that SMEDDS formulation could be an effective method for increasing the oral bioavailability of vorinostat, which is poorly water soluble.
