International Journal of Drug Delivery
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Development and in vitro evaluation of mucoadhesive microsphere carriers for intranasal delivery of betahistine dihydrochloride.
Get PDFThe aim of the present work was to formulate and evaluate betahistine-loaded chitosan microspheres intended for nasal delivery with focus on their mucoadhesive properties. Betahistine-loaded chitosan microspheres were obtained via W/O emulsion solvent evaporation technique and were characterized for particle size, surphace morfology and entrapment efficiency. FTIR spectroscopy was carried out to evaluate drug-polymer interaction and powder X-ray diffractometry was applied to investigate crystallinity transformations. Tensile studies were carried out using sheep nasal mucosa to evaluate in vitro mucoadhesion. Drug release into phosphate buffer saline pH 7.4 was performed and dissolution profiles of the formulations were obtained. The results showed that the microspheres were spherical in shape having smooth surface and mean particle size of 3.82 µm to 7.69 µm which is appropriate for optimum deposition in the nasal cavity. The mean particle size increased when chitosan solutions with higher viscosity were used. In vitro mucoadhesion studies indicated that chitosan microspheres had good mucoadhesive properties and could adequately adhere to nasal mucosa. It was observed that polymer concentration enhancement led to increased mucoadhesive strength. Betahistine release studies from the microspheres showed similar and slightly icreasing dissolution profiles. Acording to the obtained results, betahistine-loaded chitosan microspheres prepared by solvent evaporation method proved to be capable of sustained release and could be used via nasal route as an alternative to oral administration
One-Pot Multicomponent Synthesis of β-Acetamido Ketones Using BF3-Et2O as Catalyst
Get PDFStarting from different ketones 1a-1f, aldehyde 2a-2g, and acetonitriles 3a-3d we synthesize some bioactive β- Acetamido carbonyl compounds 4a-4h. We also attempted to synthesize these compounds by using phenylacetone and deoxybenzoins in place of ketones to afford the products 4i-4j. 1H-NMR spectra are presented. On the basis of QSAR studies, some compounds were tested for their anti-thrombotic activity in mice. Compound 4f, 4h and 4j were found to exhibit less percentage protection
CHITOSAN NANOPARTICLES - AN EMERGING TREND IN NANOTECHNOLOGY
Get PDFThe application of nanotechnology for the treatment, diagnosis, monitoring, and control of biological systems has recently been determined by the National of Health (NIH) as nanomedicine. The strategy of Nanoparticle delivery plays a significant impact on global Pharmaceutical planning and marketing. Polymeric nanoparticles are used to control the drug release, to improve the dissolution of poorly soluble drugs in addition to improve the bioavailability of degradable substances such as protein. They also enhance the uptake of hydrophilic substances across the epithelial layers and have the potential for intracellular drug delivery. The submicron size range of nanoparticles is not only suitable for parenteral application but also applicable for mucosal routes of administration, i.e., oral, nasal, and ocular mucosa which are non-invasive route. Thus nanoparticle formulations are more advantageous over traditional dosage forms. The main aim of the present review deals with the nanoparticles of chitosan, which is a natural and bio-degradable polymer. The review focuses on the isolation, purification, characteristic features, derivatives of chitosan, preparation techniques, evaluation methods and applications of chitosan nanoparticles
Encapsulation of Lornoxicam into spermaceti microspheres and comparative bioavailability study
Get PDFIn this study, Lornoxicam (LX) loaded spermaceti (SC) microspheres were prepared using meltable emulsified dispersion cooling induced solidification technique and the bioavailability of the marketed product (Flexispaz® capsule-reference-product A) was compared with the optimized formulation (lornoxicam loaded spermaceti microspheres–test–product B). Morphological studies of wax microspheres were evaluated using scanning electron microscopy (SEM). The SEM images showed the spherical shape of wax microspheres and more than 97% of the isolated microspheres were in the size range 309-317 μm. Differential scanning calorimetry (DSC), Fourier transforms infrared (FTIR) spectroscopy and stability studies showed that the drug after encapsulation with SC microspheres was stable and compatible. A single dose, randomized, complete cross over study of LX (8mg) microspheres were carried out on 10 healthy male and female Albino sheep’s under fasting conditions. Plasma LX concentrations and other pharmacokinetic parameters obtained were statistically analyzed. Based on this study, it can be concluded that drug loaded LX microspheres and Flexispaz® capsule are bioequivalent in term of the rate and extent of absorption.Key words: Lornoxicam; Wax microspheres; Release kinetics; Bioavailability; Bioequivalence
FORMULATION AND IN VITRO CHARACTERIZATION OF ACECLOFENAC SUSTAINED RELEASE PELLETS PREPARED BY SUSPENSION LAYERING TECHNIQUE USING SUGAR SPHERES
Get PDFAbstract: The present work deals with the aceclofenac pellets prepared by suspension layering technique, using sugar spheres with various concentrations of ethyl cellulose and kollicoat SR-30D as enteric coating materials. Prepared pellets were evaluated for physical characteristics which showed excellent flow properties. Formulation F8 with the maximum drug content of 97.17% showed a prolonged in vitro drug release till 10hr when compared with the pure drug. The optimized formulation showed particle size distribution of 546µm.Further stability studies performed according to the ICH guidelines also showed no change in the drug content and property during the shelf life of 3months at prescribed RH and temperature conditions. Keywords: Aceclofenac, suspension layering, enteric coating, pellets
Comparison of Freeze Drying and Spray Drying Methods of Haruan Extract
Get PDFHaruan extract has a big potential as an active pharmaceutical ingredient for various medical conditions. However, instability of the liquid extract at room temperature has been a hindrance in the formulation stage of the preparation. Thus, dried Haruan extract has been produced using freeze drying and spray drying methods. In the spray drying method, a prototype of a spray dryer equipped with an ultrasonic atomizer was used with a different ultrasonic frequency. The spray dried extract showed better physical properties when compared to the freeze dried extract; with smaller size and narrower particle size distribution in the higher ultrasonic frequency. Voluminous flakes of the dried extract were produced in the freeze drying method while spray drying method produced almost spherical shape of particles. No structural changes in the secondary protein structure were seen regardless of the method
Evaluation of Dikamali as a Tablet Binder in Zidovudine Tablets
Get PDFThe aim of the present study is to evaluate the gum, Dikamali, as a tablet binder employing zidovudine as a model drug. Zidovudine tablets were prepared by wet granulation technique using Dikamali as a tablet binder. The Dikamali was used in wet form and dry form. Granules were evaluated for pre-compression parameters: tapped density, bulk density, compressibility index, hausner ratio, and angle of repose. All the parameters were found to be within the acceptable limits. The tablets were evaluated for hardness, friability, weight variation, disintegration, content uniformity, and dissolution. For the formulations F1-F3D; F1-F3W; F4-F7 (see Table 1) the parameters of friability, disintegration time, and hardness were measured and their values range from 0.57-0.73% (w/w), 0.83-0.97% (w/w), 0.69-0.99% (w/w); 12-13 min, 10-12 min, 10-12 min; and 5-6.9 kg/cm2, 4.5-5.1 kg/cm2, 4.1-5.2 kg/cm2; respectively. The binding efficacy of Dikamali was compared with the standard binders, starch mucilage and polyvinyl pyrrolidone, using dissolution studies. The binders, Dikamali and starch, were compared at similar concentrations [2.5% (w/v), 5% (w/v), and 7.5% (w/v)], and the finalized formulation (F1D) was compared with a 10% (w/v) concentration of starch mucilage and a 10% (w/v) concentration of polyvinyl pyrrolidone (PVP). Dikamali [2.5% (w/v)] in dry form (i.e. F1D) showed the same percent drug release as that of the 10% (w/v) of starch mucilage and of polyvinyl pyrrolidone. In conclusion, Dikamali could well be used as a binding agent in the formulation of tablet dosage forms, and Dikamali is more effective in dry form than the wet form
Preparation and Characterization of Benzathine Penicillin G Solid Dispersions Using Different Hydrophilic Carriers
Get PDFSeveral technical factors related to penicillin G intramuscular injection can affect its bioavailability and hence reduce the efficacy of rheumatic fever prevention program. When small amount of diluent is used, the powder is not completely dissolved and the thick suspension frequently causes obstruction of injection needle. The study aimed to characterize the solid-state properties of solid dispersion systems of benzathine penicillin G (BPG) prepared with hydrophilic carriers by applying solvent evaporation method. The results of spectroscopic studies; Fourier transform-infra red (FTIR), Nuclear Magnetic Spectroscopy (1HNMR) and Differential Scanning Calorimetry (DSC) revealed no chemical interaction between the drug and carriers. No significant changes in drug crystalline state were observed by X-ray diffraction and Scanning Electron Microscope (SEM) studies, even with using amorphous carriers; polyvinyl pyrrolidone (PVP-K30) and hydroxypropyl methylcellulose (HPMC). All the prepared solid dispersions demonstrated 76-93% yield and % drug content dependent on the polymer type and concentration. The hydrophilic polymers demonstrated potential effect on improving the flowability, wettability and dissolution characters of the drug. The results revealed that it is possible to enhance the dissolution rate of BPG (hydrophobic drug) by increasing the surface area of the drug adsorbed on the surface of hydrophilic polymer by solid dispersion method. Finally, solid dispersion BPG: PEG 4000 at ratio 50:50 gave uniform flowability of the powder (around 30), wettability (12 min) and faster dissolution rates among all the formulations. Thus, it was selected as the best formulation in this study
Novel Biocompatible Honey Hydrogel Wound Healing Sponge for Chronic Ulcers
Get PDFThere is an ever-present need for non-allergenic antibacterial and antifungal wound dressing with a superior healing property for chronic ulcers. Among the entire modern wound healing dressings, hydrogel has a good capacity to donate moisture or absorb exudate and thereby providing a moist environment to facilitate wound healing process and at the same time protect the wound too. In the present study, povidne iodine loaded acrylamide based biocompatible biodegradable hydrogel dressings incorporating alginate, chitosan and gelatin showed good fluid absorbance capacity. The addition of honey showed improved tensile strength and moisture absorbance capacity of the hydrogel sponge. Apart from tensile strength, all the formulations were evaluated and compared for thickness, % elongation, folding endurance, swelling ratio, % of drug loading, thrombus formation, haemolysis assay and dispersion characteristics. Hydrogel containing chitosan and alginate showed better results in terms of tensile strength 4323gm/mm2, drug loading (27.17 %), thrombus formation (0.002 gm), drug release (97.99 %) and other parameters compared to gelatin based hydrogel. Wound healing study using well established wistar rat model showed complete healing of wound i.e. 98.28 % within 12 days. Povidone-Iodine and honey loaded acrylamide hydrogel with chitosan and alginate presented a very promising wound healing dressing. This honey hydrogel dressing can be a good alternative for infected chronic wounds and diabetic foot ulcers
Synthesis, Characterization And Antimicrobial Activity Of Novel Substituted Aryl- 1,3,4-Oxadiazolo-[3,2-A]-1,3,5-Triazine Derivatives
Get PDFBioactive heterocyclic rings 1,3,4-oxadiazole and 1,3,5-triazine are fused with expectation of enhanced biological activity of the newly synthesized compounds. Hence Synthesized fused heterocyclic compounds as a substituted aryl- 1,3,4-oxadiazolo-[3,2-a]-1,3,5-triazine derivatives The structures of all the compounds were confirmed by physical and spectral analysis. The newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains and fungal strains. Some of these compounds have shown significant antibacterial and antifungal activity