To analyze population pharmacokinetics of Propofol in Indian patients after single bolus dose of Propofol using WINNONLIN program.
Population pharmacokinetics of Propofol was investigated in Indian ...subjects in 26 elective surgical patients (14 males and 12 females) following single bolus dose of 2 mg/kg propofol. A total of 364 samples were estimated by High Performance Liquid Chromatography and pharmacokinetic parameters were derived using WINNONLIN (5.2). The effect of demographic characters of the study population on pharmacokinetic parameters was investigated.
Three-compartment model was used to describe the pharmacokinetic data of Propofol in Indian subjects. Initial volume of distribution (V1) clearance (Cl) and steady state volume of distribution (Vd(ss)) was 13.5 ± 3.3 l, 1.08 ± 0.42 l/min, and 77.69 ± 48.0 l, respectively. Body weight best described the volume of central compartment (V1) as well as elimination clearance (P<0.01).
Pharmacokinetics of Propofol in young healthy Indian subjects show lower volume of distribution and clearance as compared with most of the western data. Body weight best describes the V1, Vd(ss), and Clearance in this group.
Prednisolone-loaded bovine serum albumin (BSA) nanospheres prepared by pH-coacervation were evaluated regarding recovery, drug entrapment efficiency, particle size, shape, surface morphology, in ...vitro drug release profile, and in vivo distribution. The method of analysis was validated in terms of accuracy, precision, and repeatability. No significant change in the drug's chemical integrity was observed when incorporated in the nanospheres. It was observed that the average particle size and drug entrapment efficiency of the nanospheres increased with the increase in drug loading. All the batches exhibited biphasic drug release with an initial burst effect followed by gradual steady release. The higher the drug loading, the greater was the burst effect. The mechanism of prednisolone release from the nanospheres was found to be due to diffusion and erosion as observed by fitting the release data in different models. The drug's in vivo distribution was found to be highest in the liver followed by the spleen and lungs. Stability studies indicated that nanosphere formulations should be stored at 4 +/- 2 degrees C.
Phase-sensitive in situ gel forming controlled release formulations of cyclosporine were prepared using poly (lactide-co-glycolide) and a solvent system consisting of various proportions of benzyl ...benzoate and benzyl alcohol. Uniformity of content of cyclosporine in the formulation and in vitro release samples was determined by radio immune assay (RIA). FTIR and CD spectroscopy ratified the conformational stability of cyclosporine in the formulation and in vitro release samples, respectively. Rheological properties of the formulations, assessed under isothermal conditions, showed dilatant behavior of all the formulations. In vivo studies were carried out on the optimized formulations vis-à-vis pure cyclosporine in rats and drug levels were monitored for 13 days. Mean plasma concentration of cyclosporine was calculated for all the animals and pharmacokinetic parameters were determined using Win NonLin software. The studies construed better regulation of plasma drug levels with the optimized formulation vis-à-vis routine once-a-day administration of cyclosporine. The subcutaneous tissues, further subjected to histopathological examinations ascertained the biocompatibility of the formulation.
Opisana je priprava albuminskih nanočestica s paklitakselom (PTX) metodom desolvatacije. Za pripravu je korišten goveđi serumski albumin (BSA) i 32 potpuni faktorijalni dizajn (FFD). Pomoću fotonske ...korelacijske spektroskopije određena je veličina čestica, dok je površina čestica proučavana pretražnom elektronskom mikroskopijom (SEM) i transmisijskom elektronskom mikroskopijom (TEM). Nadalje, određena je učinkovitost kapsuliranja, zeta potencijal i iskorištenje. Linearno modeliranje odzivnih površina (RSLM) upotrebljeno je za predviđanje optimalne formulacije. Različiti modeli primijenjeni su za određivanje mehanizma oslobađanja iz PTX nanočestica. Proučavan je utjecaj omjera lijeka i polimera na profil oslobađanja i njegova upotrebljivost za predviđanje optimalne formulacije. Mogućnost ciljane isporuke u mozak preliminarno je ispitana in vivo na miševima.
Silymarin is a powerful free radical scavenger, anti-inflammatory and immune system modulating agent which can be effectively used for the treatment of various skin ailments. The present research ...work emphasizes on establishing the antiphotoageing potential of Silymarin biochemically followed by the development of a nanotailored topical carrier system of Silymarin for its improved therapeutic effect by enhancing its skin retention and minimizing systemic delivery. Silymarin laden nanoemulsion was formulated and optimized using Quality by Design (QbD) concept. Based upon the quality target product profile (QTPP), critical quality attributes (CQAs) and critical material attributes (CMAs) were finalized. D-optimal mixture design was employed to find the points of the CMAs in the design space. Globule size and percentage cumulative drug release were set as CQAs. The nanoemulsion was gellified and the obtained nanoemulgel was further assessed for physical and skin permeation characteristics. From the permeation study it was found that the nanoemulgel showed better skin permeation and skin retention features of Silymarin in contrast to its conventional gel. Further, the outcome of Confocal Laser Scanning Microscopy (CLSM) advocated the efficiency of nanoemulgel as Rhodamine B was highly spotted in the deeper skin layers. Hence, the developed Silymarin loaded nanoemulgel proved to be a promising topical delivery system for improved antiphotoageing activity.
Display omitted
Cubosome is a biocompatible, thermodynamically stable and bioadhesive drug carrier that is prepared from certain amphiphilic lipids and surfactants when mixed in a definite ratio. Structurally, they ...are selfassembled nano-constructed liquid crystalline particles comprising three-dimensionally arranged bicontinuous as well as nonintersecting lipid bilayers that give them a honeycomb-like appearance. Morphological characterization through SAXS (small-angle X-ray scattering) and cryo-TEM (cryo-transmission electron microscopy) revealed that they are square and round shaped particles in the nanometer range. These carriers have two separate aqueous regions and a large interfacial area that allow them to carry a variety of bioactive molecules having hydrophobic, hydrophilic or amphiphilic behavior. One of either two strategies i.e., top-down or bottom-up methods can be adopted to prepare these cubic structures. A number of dispersion techniques like sonication, spray drying, high-pressure homogenization or spontaneous emulsification can be adopted to prepare cubosomes. Their characteristics and benefits like multicompartmental structure, high drug loading, simple and convenient method of preparation, use of biodegradable lipids such as glycerol monooleate, encapsulation of hydrophilic, hydrophobic and amphiphilic moieties, targeted and controlled release make them versatile bioactive carriers that can be administered through multiple biological routes like topical, transdermal, parenteral, and oral. Cubosomes have appreciable applications in various fields especially in the pharmaceutical industry where they are used as potential bioactive carriers. Molecules like paclitaxel, oligonucleotide, δ-amino-levulinic acid, bovine serum albumin, etc. can be easily delivered through this system. This article provides a detailed note on the structure of cubosomes, ingredients and techniques used for their preparation, mechanism of drug release, applications and routes of drug administration, their formulations, patent review and market scenario.
In recent decades, nanoscience and nanotechnology have played a revolutionary role in
the therapeutic domain. Manipulation of atoms and molecules at the nanometric scale endows biomaterials
with ...specific physicochemical properties. Skin being the largest organ of the human body
and an extensively exploited route for drug delivery, is one of the primary sites for exposure to
nanoparticulate matter. Skin care products and cosmetics also constitute a major source of exposure
to metallic nanoparticles. Metallic nanoparticles are widely used for therapeutic, diagnostic
and cosmetic purposes. The potential risks associated with their use in modern medicine are a subject
of extensive research. The present article aims to discuss the toxicity concerns associated with
the use of metallic nanoparticles in dermatological products, and provide an overview of their in
vitro and in vivo methods of nanotoxicity assessment, as per OECD guidelines. It also presents a
concise account of the lacunae in the existing guideline, which need to be addressed in order to
adapt the prescribed tests to the testing of nanoparticles. The review also gives an insight into the
gaps in the in vitro, in vivo correlation of data furnished by various research groups. It provides a
glimpse of important regulatory aspects applicable to the evaluation of topically applied nanoparticulate
systems. In the end, it discusses the challenges and future perspectives in order to strengthen
the scientific investigations in this domain.
PDF
