Optimized Microsphere Formulation Research Articles

Formulation and evaluation of emulgels loaded with microspheres containing Baricitinib

The main objective of the present research work was to formulate and evaluate transdermal gel loaded with microspheres of Baricitinib to increase bioavailability and to reduce the dosing frequency and to improve patient compliance. Gel loaded with microspheres of Baricitinib was prepared by taking different ratios and grades of Carbopol polymers. The prepared formulations (F1–F9) were evaluated for pre-formulation studies, percentage yield, particle size, content Uniformity, drug content entrapment efficiency and in vitro dissolution studies. The optimized gel loaded with microspheres of F8 formulation (drug: Carbopol 974polymer in 1:1 ratio) is more effective compared to all formulations. The prepared gel showed acceptable physical properties such as particle size of (126.5 microns), percentage yield of (96.5%), content uniformity (97.8), and drug content entrapment efficiency (90.5%). In vitro dissolution studies have shown 100.1% drug release in 12 h. With the optimized formulation Baricitinib emulgels are formulated using different grades and ratios of Carbopol and optimized microsphere formulation F8. The Emulgel formulation F7 showed the acceptable results with a yield of 92.3%, Drug content (100.2%), Spread ability (13.38 g.cm/s), Viscocity (112.3 cP), pH off 6.05 and it was observed that formulation F7 showed 100.2% drug release within 12 hours. All the results show that the gel loaded with microspheres of Baricitinib can be effectively used for the treatment of viral infections like small fox.

OPTIMIZATION OF COMPONENT VARIABLES BY STATISTICAL APPROACH FOR DESIGN OF CHRONOTHERAPEUTIC DOSAGE FORM FOR HYPERTENSION

Objective: Blood pressure (BP) pursues circadian rhythms projecting its highest values during early morning and lowest during night. The aim of the present investigation was to design a newer programmable chronotherapy based capsule system containing delayed release microspheres of losartan potassium for effective management of hypertension.
 Methods: First, the microspheres were prepared with Eudragit RS100 by optimization technique through the application of Design Expert® software. The optimized microsphere formulation was filled in a capsule shell, and these shells were coated with 10% w/v Eudragit L100:Eudragit S100 (in ratio 1:2), in isopropyl alcohol: water as solvent system, to provide the necessary delay in emptying of capsule content. The whole capsular system was evaluated by various characteristic formulation parameters. Validation of optimization model and statistical interpretation of results was done using analysis of variance.
 Results: The results indicated that the optimized triple coated capsule shells showed an extended release of drug from microspheres after a lag time of 4 h.
 Conclusion: Conclusively, the chronotherapeutic system of losartan potassium was successfully developed to be dosed at bedtime that could benefit from the known circadian rhythms of the disease to control the BP for once a day therapy

PREPARATION AND EVALUATION OF CHITOSAN SODIUM ALGINATE CARBAMAZEPINE MICROSPHERES

ABSTRACTObjective: The objective behind our study is that a mucoadhesive rectal hydrogel chitosan sodium alginate carbamazepine (CBZ) microspheres forthe purpose of controlled release for the treatment of epilepsy to avoid the possible side effects.Methods: The study was conducted to formulate controlled release chitosan sodium alginate CBZ microspheres with the dispersion of CBZ into thenatural polymers chitosan and sodium alginate forming microspheres conducting along with their evaluation studies.Results: The formulated microspheres were subjected to various evaluation parameters, and all the physical parameters examined are within theacceptable limits. Further, the optimized microsphere formulation (CM5) was characterized. Hence, the developed optimized microsphere formulation(CM5) seems to be a viable substitute to conventional drug delivery system for the effective management of epilepsy.Conclusion: The prepared formulation also provides a desired CBZ loaded sodium alginate microspheres with the controlled release drug delivery.Keywords: Carbamazepine, Sodium alginate microspheres, Particle size.

Development of Reconstitutable Suspension Containing Aceclofenac Micro particulates

A reconstitutable sustained release suspension of micro particulate system of aceclofenac was formulated by solvent evaporation technique. Biocompatible polymers like ethyl cellulose and Eudragit RS-100 were used to prepare microspheres. The formulated microspheres were characterized for particle size, surface morphology, drug-polymer compatibility studies, differential scanning calorimetric analysis, XRD studies, SEM studies, percentage drug entrapment efficiency and in-vitro drug release studies. The prepared microspheres were found to be free flowing and particle size of the microspheres were found to be in the range of 144.93-301.26 µm. SEM studies indicated that the microspheres were spherical in shape. In-vitro drug release studies showed a sustained release of drug over a period of 9 hours. The reconstitutable suspension of aceclofenac microparticulates was prepared using xanthan gum in various concentrations of 1.5, 2.0 and 2.5 % w/v as suspending agents. The suspensions were evaluated for reconstitutability, viscosity, sedimentation rate, percent drug content and in-vitro dissolution studies. The optimized microsphere formulation showed Peppas model to be the most appropriate drug release mechanism. The prepared sustained release suspension is capable of sustaining the drug release over a period of 10 hours. Stability studies showed no significant change in drug content in the optimized formulation after 6 months. The results obtained in this work thus suggest that a microparticulate dosage form of aceclofenac can be successfully designed to provide sustained drug delivery.

Preparation, characterization and pulmonary pharmacokinetics of xyloglucan microspheres as dry powder inhalation

The purpose of the present investigation was to prepare microspheres using xyloglucan as the polymer and to evaluate them for pulmonary delivery of Montelucast. Xyloglucan microspheres were prepared using spray-drying technique employing lactose monohydrate as carrier for dry powder inhalation. The formulation of microspheres was optimized using response surface methodology. Multiple response surface simultaneous optimizations using desirability approach were use to find optimal formulation. In vitro characterization of optimized microsphere formulation demonstrates its suitability as dry powder inhalation. It found to provide high and prolonged drug concentration within lungs after pulmonary administration in animal model.

Design, Characterization and Pre-Clinical Evaluation of Aceclofenac Loaded Algino-gelatin Microspheres for Targeted Drug Delivery

Multiple-unit type oral modified drug delivery system of aceclofenac was developed by ionotropic gelation method for targeted drug delivery and to reduce the chances of side effects. Various batches of microspheres were developed by ionotropic gelation method using single and blends of polymers. Along with usual physical properties, the microspheres were also subjected to enteric nature, in-vitro drug release and mucoadhesion studies to investigate a possible sustained drug release and their use in in-vivo as a gastro-protective system for aceclofenac. It was observed that prepared microspheres could be able to restrict the drug release in stomach region and prolong the drug release by adhering on to the intestinal mucosa. In vitro drug release suggested a combination of drug diffusion and spheres erosion could be the release mechanism and it was also found that blend of polymers is more effective in sustaining the drug release than either polymer. Optimized microsphere formulation suggested 71.03 ± 4.94 % edema inhibition at 12 hours and shelf life of about 2.32 years at room temperature. Algino-gelatin multiunit dosage system exhibits promising properties for once daily targeted release form of aceclofenac in order to reduce the side effects and enhance the patient’s compliance. Keywords: Algino-gelatin microspheres, enteric nature, gastro-protection, in-vivo study, mucoadhesion, targeted release.

Novel Carboxymethyl Chitosan Microspheres for Controlled Delivery of Chelerythrine

Novel carboxymethyl chitosan (O-CMCS) microspheres containing an anti-tumor drug chelerythrine (CHE) have been successfully prepared by an emulsion crosslinking method using glutaraldehyde. The optimized microsphere formulation was characterized for particle size, shape, morphology, crystallinity and in vitro drug release. Results for mean particle size, drug loading content, entrapment efficiency and in vitro drug release of chelerythrine loaded microspheres were found to be 12.18 μm, 4.08%, 54.78% and 35.30% at pH 7.4 in 20 h, respectively. The optimized microspheres had an imperfect crystalline lattice and a spherical, rough morphology and the CHE release from O-CMCS microspheres followed the Higuchi matrix model. All these results suggested that O-CMCS microspheres are a promising carrier system for controlled drug delivery.

Formulation optimization of chelerythrine loaded O-carboxymethylchitosan microspheres using response surface methodology

The aims of this investigation were to develop a procedure to prepare chelerythrine (CHE) loaded O-carboxymethylchitosan (O-CMCS) microspheres by emulsion cross-linking method and optimize the process and formulation variables using response surface methodology (RSM) with a three-level, three-factor Box–Behnken design (BBD). The independent variables studied were O-CMCS/CHE ratio, O/W phase ratio, and O-CMCS concentration, dependent variables (responses) were drug loading content and encapsulation efficiency. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The process and formulation variables were optimized to achieve maximum drug loading content and entrapment efficiency by the desirability function. The optimized microsphere formulation was characterized for particle size, shape, morphology and in vitro drug release. Results for mean particle size, drug loading content, entrapment efficiency, and in vitro drug release of CHE-loaded O-CMCS microspheres were found to be of 12.18μm, 4.16±3.36%, 57.40±2.30%, and 54.5% at pH 7.4 after 70h, respectively. The combination use of RSM, BBD and desirability function could provide a promising application for O-CMCS as controlled drug delivery carrier and help to develop procedures for a lab-scale microemulsion process.

PLGA 미립구를 이용한 새로운 단회 접종 항원 전달 시스템의 개발

A promising approach to the development of a new single-step vaccine, which would eliminate the requirement for multiple injections, involves the encapsulation of antigens into microspheres. Biodegradable poly(lactide-co-glycolide) (PLGA) microspheres gave us a bright insight for controling antigen release in a pulsatile fashion, thereby mimicking two or tree boosting injections. However, in spite of the above merits, the level of immunization induced by a single-shot vaccination is often lower tan two doses of alum-adsorbed antigen. Therefore, optima modification of the microsphere is essential for the development of single-step vaccines. In the review, we discuss the stability of antigen in microsphere, safety and non-toxic in human and encapsulation technology. Also, we attempted to outline relevant physicochemical properties on the immunogenicity of microsphere vaccine and attainment of pulsatile release pater by combination of different microsphere, as well as to analyze immunological data associated with antigen delivery by microsphere. Although a lot of variables are related to the optimized microsphere formulation, we could conclude that judicious choice of proper polymer type, adjustment of particles size, and appropriate immunization protocol along with a suitable adjuvant might be a crucial factor for the generation of long-lasting immune response from a single-step vaccine formulation employing PLGA microsphere.