Formulation and In-Vitro Evaluation of Rosuvastatin Nanoemulsions

Introduction: Rosuvastatin (ROS) calcium is the latest synthetic drug in the statin group that has an anti-hyperlipidemic activity. It is available as tablets, and its poor aqueous solubility, slow dissolution rate and low-absorption extent result in less than 20% bioavailability and about 80% being excreted unchanged in the feces without absorption. The present study aimed at developing an optimal oral nanoemulsion formulation containing rosuvastatin using different proportions of oil and surfactant system for enhancing its water solubility and bioavailability. Methods and results: The solubility of ROS in different oils, surfactants and co-surfactants was tested. Based on the solubility study, liquid formulations were prepared using Arachis oil as oil phase and Tween 80 as surfactant and polyethylene 400 as co-surfactant. Pseudo-ternary phase diagrams were developed and various nanoemulsion formulations were prepared and evaluated for globule size, zeta potential, and emulsion properties. The formulations were subjected to different thermodynamic stability studies such as centrifugation, heating-cooling cycle and freeze-thaw cycle, to avoid the selection of metastable formulations. Transmittance study and in-vitro dissolution studies were carried out. An optimal nanoemulsion system was successfully developed with the droplet size of 260 nm and a composition of (Arachis oil; 20%), Tween 80 (40%) and PEG 400 (40%). The cumulative percentage drug release from optimal nanoemulsion formulation was found to be 93.29±1.11% for 50 minutes, which was significantly higher than the drug suspension (43.42±1.30%). Thus, in vitro results reveal that the prepared nanoemulsion formulations showed improved solubility of ROS. Conclusions: Nanoemulsion formulations of ROS represent a promising novel formula with a higher dissolution rate when compared to the drug in suspension. &nbsp

Ex-situ and in-situ post-photosynthesis of silver nanoparticles on polyamide fabric using daylight irradiation

Silver nanoparticles (AgNPs) have been ex-situ post-synthesized in an aqueous solution and in-situ synthesized on polyamide fabric through a simple chemical reduction method by using silver nitrate (AgNO3), stannous chloride (SnCl2) and cetyltrimethylammonium bromide (CTAB) under daylight irradiation. SnCl2 and CTAB act as reducing and stabilizing agents in the colloidal silver nanoparticles solution respectively. Post in-situ synthesis of Ag NPs have been carried out on polyamide fabric by spraying solution of AgNO3, CTAB and SnCl2 on the fabric and then irradiating under daylight for 2 h. Ag NPs solutions and Ag NPs loaded polyamide fabrics are characterized by UV-vis spectroscopy, dynamic light scattering (DLS), X-ray diffraction (XRD) and scanning electron microscopy (SEM). Appearing a strong plasmon resonance peak at 400 nm in UV-visible spectrum, XRD patterns and SEM images are found to clearly confirm the formation of silver nanoparticles. The UV-vis spectra also confirm no Ag NPs formation without daylight irradiation

Učinci adheziva osjetljivih na tlak i kemijskih promotora na permeaciju fentanila kroz kožu štakora

Drug-in-adhesive patches (DIAPs) of fentanyl were formulated using various pressure sensitive adhesives (PSAs) and various chemical permeation enhancers (CPEs). The effects of the PSAs and CPEs on skin permeation of fentanyl from DIAPs were evaluated using modified jacketed Franz diffusion cells fitted with excised rat abdominal skin. It was demonstrated that permeation rate or steady state flux (Jss) of the drug through the excised rat skin was dependent on the viscosity and type of acrylic PSA as well as the type of CPE. Among different acrylic PSAs, Duro-Tak® 2054 and Duro-Tak® 2516 showed the highest Jss of 1.95 μg cm-2 h-1 and the lowest Jss of 1.43 μg cm-2 h-1, respectively. Among the various CPEs used, propylene glycol and polyethylene glycol 400 showed 1.61 and 1.18, the highest and lowest enhancement ratio (ER) on the skin permeation of fentanyl, respectively. Oleic acid and cetyl alcohol moderately increased the skin permeation of fentanyl. It was also shown that increasing the concentration of CPE led to reduction in adhesion property of PSA as measured by 180° peeling strength test. Moreover, it was found that the permeation rate increased as the fentanyl loading increased from 1 to 3%. The skin permeation rate of fentanyl did not increase significantly beyond 3% drug loading. It was concluded that PG as a CPE and cosolvent in 10% m/m with 3% fentanyl loading in Duro-Tak 2054 showed an effective monolithic DIAP for the development of a transdermal therapeutic system for fentanyl.Pripravljeni su transdermalni adhezivni flasteri fentanila (DIAPs) koristeći različite adhezive osjetljivih na tlak (PSAs) i kemijske promotore permeabilnosti (CPEs). Njihovi učinci na permeabilnost fentanila evaluirani su pomoću modificirane Franzove difuzijske ćelije s membranom od kože s abdomena štakora. Brzina permeabilnosti (Jss) ovisi o viskoznosti i vrsti akrilnih adheziva i o vrsti promotora. Najveća vrijednost Jss = 1,95 μg cm-2 h-1 postignuta je s Duro-Tak® 2054, a najmanja (Jss = 1,43 μg cm-2 h-1) s Duro-Tak® 2516. Među različitim promotorima propilen glikol i polietilen glikol 400 pokazali su najveći (1,61) i najmanji (1,18) omjer poboljšanja (ER) permeabilnosti. Oleinska kiselina i cetil alkohol umjereno su povećali permeabilnost fentanila. Za mjerenje adhezivnih svojstava upotrebljena je "metoda ljuštenja". Povećanje koncentracije CPE smanjilo je adhezivna svojstva PSA. Kada je udio fentanila u flasteru povišen s 1 na 3%, brzina permeabilnosti se povećala, dok daljnje povećanje udjela fentanila nije značajno utjecalo na brzinu. Pripravak s 10% propilen glikola i 3% fentanila u Duro-Tak 2054 pokazao se kao učinkoviti transdermalni terapijski sustav za fentanil

Effect of Amino-Functionalization on Insulin Delivery and Cell Viability for Two Types of Silica Mesoporous Structures

Inorganic Mesoporous Structures Are a Class of Novel Biomaterials that Have Shown Practical Applications in Delivery of a Variety of Therapeutic Agents. in the Present Study, Two Mesoporous Structures Were Prepared, and the Effect of Surface Modification on their Insulin Delivery and in Vitro Cytotoxicity Was Evaluated. Morphological and Structural Characterizations of Silica Particles Were Accomplished by Different Analytical Techniques, Including Scanning Electron Microscopy, X-Ray Diffraction, Fourier Transform Infrared Spectroscopy (FTIR), and Brunauer–Emmett–Teller (BET) Surface Area Analyses. the Drug Loading Capacity and in Vitro Drug Release Behavior of Silica Structures Were Investigated under Simulated Gastrointestinal Conditions and Phosphate-Buffered Saline Solution using FTIR and UV–Vis Spectroscopy. in Vitro Cytotoxicity Evaluation Was Carried Out Via MTT Assay. Results Showed that the Morphology of MCM-41 Was Round, While SBA-15 Was Wheat Like, Both Possessed Almost Homogeneous Size Distribution. Also, Modification with Amine Did Not Influence the Morphology and Structure of the Particles. Both MCM-41 and SBA-15 Particles Were Found to Have Narrow Pore-Size Distributions of 2.8 and 6.8 Nm, Respectively. SBA-15 Particles Demonstrated a High Insulin Loading Capacity of About 15.1 %, While MCM-41 and Modified MCM-41 (MMCM-41) Were Observed to Load Virtually No Insulin at All. the Surface Modification by Amino Groups Resulted in Higher Insulin Loading and the Slower Rate of Release for Modified SBA-15 (MSBA-15) Compared to the Non-Modified SBA-15 (SBA-15). According to the Cytotoxicity Evaluation Results, All of the Samples Showed Cytotoxicity Grade 0–1, in a Concentration-Dependent Manner. Moreover, Insulin-Loaded MSBA-15 Particles Exhibited Higher Cell Viability Compared to the Others. It Was Concluded that Amine Modification of SBA-15 Could Result in Higher Loading and Extended Release of Insulin and More Cell Viability

Pegylated niosomal nanoparticles loaded with vincristine: Characterization and in vitro evaluation

Purpose: To investigate the effect of pegylated niosomal vincristine (VCR) on enhanced performance, drug resistance and prolonged blood circulation time.Methods: Pegylated niosomal VCR was synthesized by reverse phase evaporation. The mean diameter, size distribution, and zeta potential of pegylated niosomal VCR were evaluated using a Zetasizer. The half-maximal concentration (IC50) values of pegylated niosomal VCR and standard VCR were determined using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The impact of pegylated niosomal VCR on apoptosis and cell cycle of BCL1 lymphoma cancer cells were investigated.Results: The mean diameter, size distribution and zeta potential of pegylated niosomal VCR were 220 nm, 0.4, and –18.8 mV, respectively. Cell proliferation was evaluated using the MTT assay. The IC50 values of pegylated niosomal VCR and standard VCR were 1.6 and 3.5 μg/mL, respectively, after a 24-h incubation. The cytotoxicity of pegylated niosomal VCR was twice that of standard VCR. Furthermore, flow cytometric analysis of the cell cycle showed that pegylated niosomal VCR induced greater mitotic arrest than did standard VCR.Conclusions: The findings demonstrate the effective antitumor activity of pegylated niosomal VCR compared with standard VCR.Keywords: Niosome, Anti-tumour, Polyethylene glycol, Vincristine,   Encapsulation, Lymphom

Determination of Scientific Name of Bitter “Qust”: an Important Controversial Plant Source in the Iranian Medicinal Plants Market for Neurological Complications

Background and objectives: Traditional medicine could provide a hopeful area of research to mitigate the suffering of patients. “Qust” is one of the medicinal plants that are mentioned in Persian Medicine (PM) for treatment of neurological diseases. There is diversity within the scientific name of “Qust” in different references. Some have introduced Saussurea costus (Falc.) Lipsch. (Asteraceae), while others have presented Costus speciosus (J. Koenig) Sm. (Costaceae) as “Qust”. Since “Qust” is not endemic in Iran, there is difficulty to access to the whole plant for its identification. Hence, this study has aimed to identify available bitter “Qust” which is composed of roots of the plant in the Iranian market. Methods: Macroscopic characters and microscopic properties of powders and transverse sections of specimens with essential oil analysis of the Indian and one of the Iran herbal market samples using chromatography-mass spectrometry (GC-MS) were investigated for identification of bitter “Qust”. Results: Microscopic evaluation showed presence of secretory cavities and their specific size, narrow radial rows of conducting tissue alternating with broad medullary rays in the secondary phloem and xylem, presence of inulin, absence of starch and calcium oxalate crystals in the bitter “Qust” particles. Further, positive response was observed to S. costus identifying test. In the analysis of essential oils, active components of S. costus, such as dehydrocostus lactone, were identified in the examined essential oils. Conclusion: According to the results, it could be concluded that bitter “Qust” in Iran herbal market most probably is S. costus

<i><span style="font-size:15.0pt;mso-bidi-font-size: 16.0pt;font-family:"Times New Roman";mso-fareast-font-family:"Times New Roman"; mso-bidi-font-family:Mangal;mso-ansi-language:EN-GB;mso-fareast-language:EN-US; mso-bidi-language:HI;mso-bidi-font-weight:bold" lang="EN-GB">Ex-situ</span></i><span style="font-size:15.0pt;mso-bidi-font-size:16.0pt;font-family:"Times New Roman"; mso-fareast-font-family:"Times New Roman";mso-bidi-font-family:Mangal; mso-ansi-language:EN-GB;mso-fareast-language:EN-US;mso-bidi-language:HI; mso-bidi-font-weight:bold;mso-bidi-font-style:italic" lang="EN-GB"> <span style="font-size:15.0pt;mso-bidi-font-size:16.0pt;font-family:"Times New Roman"; mso-fareast-font-family:"Times New Roman";mso-bidi-font-family:Mangal; mso-ansi-language:EN-GB;mso-fareast-language:EN-US;mso-bidi-language:HI; mso-bidi-font-weight:bold" lang="EN-GB">and <i>in-situ</i> post-photosynthesis of silver nanoparticles on polyamide fabric using daylight irradiation</span></span>

55-61Silver nanoparticles (AgNPs) have been ex-situ post-synthesized in an aqueous solution and in-situ synthesized on polyamide fabric through a simple chemical reduction method by using silver nitrate (AgNO3), stannous chloride (SnCl2) and cetyltrimethylammonium bromide (CTAB) under daylight irradiation. SnCl2 and CTAB act as reducing and stabilizing agents in the colloidal silver nanoparticles solution respectively. Post in-situ synthesis of Ag NPs have been carried out on polyamide fabric by spraying solution of AgNO3, CTAB and SnCl2 on the fabric and then irradiating under daylight for 2 h. Ag NPs solutions and Ag NPs loaded polyamide fabrics are characterized by UV-vis spectroscopy, dynamic light scattering (DLS), X-ray diffraction (XRD) and scanning electron microscopy (SEM). Appearing a strong plasmon resonance peak at 400 nm in UV-visible spectrum, XRD patterns and SEM images are found to clearly confirm the formation of silver nanoparticles. The UV-vis spectra also confirm no Ag NPs formation without daylight irradiation

A Review on Application of Phase Change Materials in Textiles Finishing

Fabric as the first and most common layer that is in permanent contact with human skin is a very good interface to provide coverage, as well as heat and cold insulation. Phase change materials (PCMs) are organic and inorganic compounds which have the capability of absorbing and releasing noticeable amounts of latent heat during phase transitions between solid and liquid phases at a low temperature range. PCMs come across phase changes (liquid-solid and solid-liquid transitions) during absorbing and releasing thermal heat; so, in order to use them for a long time, they should have been encapsulated in polymeric shells, so-called microcapsules. Microencapsulation and nanoencapsulation methods have been developed in order to reduce the reactivity of a PCM with outside environment, promoting the ease of handling, decreasing the diffusion and evaporation rates. Methods of incorporation of PCMs in textiles such as electrospinning and determining thermal properties had been summarized. Paraffin waxes catch a lot of attention due to their high thermal storage density, repeatability of phase change, thermal stability, small volume change during phase transition, chemical stability, non-toxicity, non-flammability, non-corrosive and low cost and they seem to play a key role in confronting with climate change and global warming. In this article, we aimed to review the researches concentrating on the characteristics of PCMs and new materials and methods of microencapsulation

Preparation of Saussurea costus Traditional Oil and Investigation of Different Parameters for Standardization

Background and objective: Medicinal oils are one of the most common and special dosage forms in oral and topical therapies of Persian medicine (PM). The oil of Saussurea costus (bitter qust) root is prominent topical oil with different applications in PM. In this study, the oil of bitter qust was prepared according to ancient Persian medical texts. Methods: To prepare traditional qust oil, 100 g of the root was soaked in 600 mL aqueous ethanol 25% overnight. The supernatant was then filtered and boiled in 800 g sesame oil until all water was evaporated. The essential oil of the root and volatile components of its traditional oil were extracted using hydro-distillation method in a Clevenger-type apparatus and were analyzed by gas chromatography-mass spectrometry (GC-MS) method. Total phenolics, flavonoids, tannins and polysaccharides were determined by spectrophotometric methods to evaluate the chemical parameters of traditional bitter qust oil.  Results: The content of volatile compounds in both investigated samples was determined (0.5% and 0.1% (v/w), respectively). Dehydrocostus lactone and 1, 3-cyclooctadiene were two similar main compounds in the both analyzed samples. Total phenolics (788.290±0.61 mg/L gallic acid equivalent (GAE)), flavonoids (303.2±2.52 mg/L catechin equivalent (CE)), tannins (23.97±0.52 mg/L GAE) and polysaccharides (9.240±0.13 mg/L dextrose equivalent (DE)) contents were determined. Conclusion: According to the obtained data, dehydrocostus lactone could be used for determination and evaluation of traditional bitter qust   oil