scholarly journals FORMULATION AND CHARACTERISATION OF SUSTAINED RELEASE MICROBEADS LOADED WITH ZALTOPROFEN

2019 ◽  
pp. 173-180
Author(s):  
H. C. KIRAN ◽  
DHANDAPANI NAGASAMY VENKATESH ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Calcium Chloride ◽  
Oral Bioavailability ◽  
Half Life ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Drug Entrapment Efficiency

Objective: The main aim of the present investigation was to formulate and evaluate microbeads of zaltoprofen. Zaltoprofen, a BCS class II drug used in the treatment of rheumatoid arthritis. Zaltoprofen has a shorter half-life of 2.8 h, and it is administered at a dose of 80 mg thrice a day. By encapsulating the drug into microbeads, it is expected that the release of the drug would be prolonged and thereby, it reduces the frequency of administration and better patient compliance may be improved. Methods: Gellan-chitosan and calcium chloride beads of zaltoprofen were prepared employing ionotropic gelation method using different concentrations of gellan, chitosan, calcium chloride and zaltoprofen. The microbeads were evaluated for its various Physico-chemical parameters such as particle size determination, drug entrapment efficiency, infrared spectroscopy study, differential scanning calorimetry, X-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo oral bioavailability studies. Results: The results suggested that the batch FG-II exhibited higher drug entrapment efficiency (72.42±0.013), a sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an enhanced oral bioavailability (2.4 times higher than that of pure drug), lower elimination rate (1.14 times lesser for the drug in microbeads) with prolonged elimination half-life (2.561 times higher than pure zaltoprofen). Conclusion: Zaltoprofen entrapped microbeads demonstrated as a better delivery system for the sustained release of drug and also to circumvent the drawbacks associated with conventional therapy.

scholarly journals ENHANCED ORAL BIOAVAILABILITY OF TENOFOVIR FROM IONOTROPICALLY GELLED MICROBEADS

2019 ◽  
pp. 242-250
Author(s):  
DHANDAPANI NAGASAMY VENKATESH ◽  
PREETY RAO ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Calcium Chloride ◽  
Oral Bioavailability ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Dissolution Profile ◽  
Class Iii ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Drug Entrapment Efficiency

Objective: The main objective of the present investigation was to develop microbeads of tenofovir. Tenofovir, a BCS class III drug has a poor bioavailability of 25%, and it is administered 300 mg once a day. By incorporating the drug into a microparticulate carrier, it is expected that the dissolution profile and the oral bioavailability may be increased. Methods: Reinforced gellan-chitosan and calcium chloride beads of tenofovir were prepared by ionotropic gelation method employing various different concentrations of gellan, chitosan, calcium chloride and tenofovir. The beads were evaluated for various physico-chemical parameters such as particle size determination, drug entrapment efficiency, swelling studies, infra red spectroscopy study, differential scanning calorimetry, x-ray diffraction analysis, scanning electron microscopy, in vitro drug release study, cytotoxicity study and in vivo oral bioavailability studies. Results: From the results, it can be concluded that the formulation TB-III exhibited higher drug entrapment efficiency (46.09±0.21), a higher swelling index, sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an increased oral bioavailability (1.25 times higher than that of pure drug), decreased elimination rate (1.32 times lesser for drug in microbeads) with prolonged elimination half-life (1.32 times higher than pure tenofovir). Conclusion: Tenofovir loaded microbeads demonstrated as a better delivery system for the modified release of drug and also to navigate the drawbacks associated with the conventional therapy.

scholarly journals SUSTAINED RELEASE MICROBEADS OF RITONAVIR: IN VITRO AND IN VIVO EVALUATION

2019 ◽  
pp. 189-198
Author(s):  
D. NAGASAMY VENKATESH ◽  
S. SHASHI KUMAR ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Calcium Chloride ◽  
Half Life ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Pure Drug

Objective: The main aim of the present investigation was to develop sustained release microbeads of ritonavir that has a shorter half-life (3-5 h) and requires twice a day administration. These formulations exhibit a sustained release of ritonavir that would expect to improve the therapy, better drug utilization, and patient compliance. Methods: Gellan-chitosan and calcium chloride reinforced beads of ritonavir were prepared by ionotropic gelation method employing different concentrations of gellan, chitosan, calcium chloride and drug. The prepared beads were evaluated for various physicochemical parameters such as particle size determination, drug entrapment efficiency, swelling studies, infrared spectroscopy study, differential scanning calorimetry, x-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo bioavailability studies. Results: From the results, formulation GC-II exhibited higher drug entrapment efficiency (79.65±0.012), higher swelling index, sustained drug release over a period of 24 h, increased oral bioavailability (2.07 times higher than that of pure drug) and decreased elimination rate (2.15 times lesser for ritonavir microbeads) with prolonged elimination half-life (2.15 times more than pure drug) as compared to pure drug. Conclusion: Ritonavir microbeads have demonstrated as a better delivery system for the sustained release of the drug; which may in turn circumvent the drawbacks associated with the conventional therapy.

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE MICROSPHERE-LOADED INTRANASAL GEL OF VENLAFAXINE HYDROCHLORIDE

2016 ◽  
Vol 9 (9) ◽  
pp. 139
Author(s):  
Kritika Saikia ◽  
Bhupen Kalita ◽  
Banasmita Kalita
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Venlafaxine Hydrochloride ◽  
Gel Formulations ◽  
Carbopol 934P ◽  
Mucoadhesive Microsphere

ABSTRACTObjective: The main objective of the present work is to develop and characterize a novel mucoadhesive intranasal microsphere gel formulation ofdrug venlafaxine to control the drug release through nasal mucosa and reach the target site with minimal side effect. The objectives of the studyare (1) formulation of mucoadhesive microspheres, (2) evaluation of mucoadhesive microspheres, (3) formulation of mucoadhesive microsphereloadednasal gel, (4) and evaluation of nasal gel.Methods: Preparation of chitosan microsphere: The chitosan microspheres were prepared by emulsion cross-linking method. Preparation ofmicrosphere-loaded gel: The nasal gels with varying concentrations of Carbopol 934P were prepared by dispersing required quantity of Carbopol inrequired quantity of distilled water with continuous stirring and kept overnight for complete hydration. The gel was then modified by the addition ofvarying proportion of hydroxypropyl methylcellulose (HPMC) K4M.Results: The prepared microspheres were evaluated for size distribution, surface morphology by scanning electron microscopy, entrapment efficiency,compatibility by Fourier transform infrared spectroscopy, and differential scanning calorimetry. Entrapment efficiency of all formulations was foundmore than 70%. Microsphere formulation containing drug and polymer in the ratio of 1:2.5 was found to be optimized. Optimized microsphereformulation was then incorporated in gel prepared using Carbopol 934P and HPMC. Prepared gel formulations were studied for viscosity, spreadability,and in-vitro drug release in simulated nasal conditions. Viscosity of the optimized batch of gel was recorded at 1056 centipoise. Drug release wasprolonged for the microsphere-in-gel formulations compared to the microspheres alone. For the optimized batch of gel, cumulative drug release of85.67% was found after 8 hrs.Conclusion: The results suggest that venlafaxine hydrochloride mucoadhesive microsphere-loaded nasal gel would give sustained drug release andsuperior bioavailability in the brain sites.Keywords: Venlafaxine, Chitosan, Mucoadhesive, Microsphere, Nasal gel.

scholarly journals Development and In-Vitro Evaluation of Budesonide Mucoadhesive Microspherefor Pulmonary Drug Delivery

2021 ◽  
Vol 11 (2-S) ◽  
pp. 76-81
Author(s):  
Jddtadmin Journal
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Chemical Interaction ◽  
Entrapment Efficiency ◽  
Pulmonary Drug Delivery ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.   Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.

scholarly journals Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

2021 ◽  
Author(s):  
Karam F. Abdalla ◽  
Mohamed A. Osman ◽  
Ahmed T. Nouh ◽  
Gamal M. El Maghraby
Keyword(s):  
Sustained Release ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Entrapment Efficiency ◽  
Fold Increase ◽  
Scanning Calorimetry ◽  
Time Curve ◽  
Diffusion Technique ◽  
Optimum Formulation

Abstract The oral absorption and hence the oral bioavailability of carbamazepine (CBZ) is variable even after administration of rapidly dissolving formulation. This problem was attributed to supersaturation of CBZ and transformation to the less soluble carbamazepine dihydrate (CBD). Accordingly, formulation of sustained release products of CBZ is a promising approach to overcome this problem. Microsponges is an emerging formulation which can help in this direction. The aim of this work was to optimize the composition of microsponges for better encapsulation and sustained release of CBZ for oral administration. CBZ microsponges were prepared using quasi emulsion solvent diffusion technique with varying composition of ethyl cellulose and polyvinyl alcohol (PVA). Microsponges were evaluated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction. Production yield, entrapment efficiency and surface morphology of microsponges were assessed in addition to drug release. Optimum formulation was administered orally to albino rabbits to evaluate the oral bioavailability with reference to unprocessed CBZ. The Instrumental analysis reflected the encapsulation of CBZ in amorphous or molecularly dispersed form in the microsponges. The size and entrapment efficiency of the microsponges increased with increasing polymer contents. This was associated with reduction in CBZ release. Optimum formulation enhanced the oral absorption of CBZ. This was manifested by 2.6-fold increase in the area under the plasma concentration versus time curve compared to that of unprocessed CBZ. The study introduced microsponges as promising carriers for sustained oral delivery of CBZ.

Development of Biodegradable Injectable In situ Forming Implants for Sustained Release of Lornoxicam

2018 ◽  
Vol 16 (1) ◽  
pp. 66-78 ◽  
Author(s):  
Ruby Christian ◽  
Vaishali Thakkar ◽  
Tushar Patel ◽  
Mukesh Gohel ◽  
Lalji Baldaniya ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Maximum Plasma ◽  
Sustained Drug Release ◽  
Drug Entrapment Efficiency ◽  
Ft Ir

Objective: The focus of this study was to develop in situ injectable implants of Lornoxicam which could provide sustained drug release. Methods: Biodegradable in situ injectable implants were prepared by polymer precipitation method using polylactide-co-glycolide (PLGA). An optimized formulation was obtained on the basis of drug entrapment efficiency, gelling behavior and in vitro drug release. The compatibility of the formulation ingredients were tested by Fourier transform infrared (FT-IR) spectroscopy, and differential scanning colorimetry (DSC). SEM study was performed to characterize in vivo behavior of in situ implant. Pharmacokinetic study and in vivo gelling study of the optimized formulation were performed on Sprague-Dawley rats. Stability testing of optimized formulation was also performed. Results: The drug entrapment efficiency increased and burst release decreased with an increase in the polymer concentration. Sustained drug release was obtained up to five days. SEM photomicrographs indicated uniform gel formation. Chemical interaction between the components of the formulation was not observed by FT-IR and DSC study. Pharmacokinetic studies of the optimized formulation revealed that the maximum plasma concentration (Cmax), time to achieve Cmax (Tmax) and area under plasma concentration curve (AUC) were significantly higher than the marketed intramuscular injection of lornoxicam. Stability study of optimized batch showed no change in physical and chemical characteristics. Conclusion: Lornoxicam can be successfully formulated as in situ injectable implant that provides long-term management of inflammatory disorders with improved patient compliance.

pH-Sensitive Interpenetrating Hydrogel for Eradication of Helicobacter pylori

2010 ◽  
Vol 3 (2) ◽  
pp. 924-932
Author(s):  
A K Gupta ◽  
Maurya S D ◽  
R C Dhakar ◽  
R D Singh
Keyword(s):  
Drug Release ◽  
Ph Value ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Crosslinking Process ◽  
Drug Entrapment Efficiency ◽  
Crosslinking Agents ◽  
Polymer Ratio

The interpenetrating hydrogels of clarithromycin were prepared by chemical crosslinking process using chitosan, poly (vinylpyrrolidone) and poly (acrylic acid) polymers and glutaraldehyde and N,N’-methylenebisacrylamide as crosslinking agents. The hydrogels were evaluated for FTIR analysis, differential scanning calorimetry (DSC), drug entrapment efficiency, scanning electron microscopy (SEM), swelling study, in-vitro drug release and mucoadhesive study. The formulation containing higher amount of chitosan showed greater swelling and drug release because of higher amount of NH2 as pendant group, which ionize at lower PH values. Finally, it was concluded that by appropriate modification of polymer ratio the extent of swelling and rate of drug release can be modulated. The result showed that IPN hydrogels prepared release the drug at lower PH value (PH 2.0) or in stomach thus maintaining antibiotic concentration in stomach for prolonged period of time.

scholarly journals “EFFECT OF CROSSLINKING AGENT ON DEVELOPMENT OF GASTRORETENTIVE MUCOADHESIVE MICROSPHERES OF RISEDRONATE SODIUM”

2018 ◽  
Vol 10 (4) ◽  
pp. 133 ◽  
Author(s):  
Shweta Gedam ◽  
Pritee Jadhav ◽  
Swati Talele ◽  
Anil Jadhav
Keyword(s):  
Differential Scanning Calorimetry ◽  
Particle Size ◽  
Drug Release ◽  
Calcium Chloride ◽  
Crosslinking Agent ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Scanning Electron ◽  
Polymer Ratio

Objective: The present investigation was undertaken to develop and evaluate a gastroretentive mucoadhesive microspheres of anti-osteoporosis drug risedronate sodium to enhance the residence time and drug release by studying the effect of the crosslinking agent to obtain the best formulation with reduced particle size and good in vitro mucoadhesion strength.Methods: Selected drug risedronate sodium is a potent pyridinyl bisphosphonate used for the treatment of osteoporosis, and other bone disorders. Microspheres using sodium alginate as a polymer and calcium chloride solution as a cross-linker were prepared successfully by the emulsification crosslinking method. The 23 factorial design was used to study the effects of various variables like a drug: polymer ratio, crosslinking agent concentration and crosslinking time on the particle size and in vitro mucoadhesion strength. All these formulations were evaluated for entrapment efficiency, percentage yield and cumulative drug release. F1 batch was selected as best formulation and evaluated for scanning electron microscopy, fourier transforms infrared spectroscopy, differential scanning calorimetry, stability study.Results: Design batches were evaluated for percent yield (61.29-89.33%), % entrapment efficiency (42.25±0.620-62.58±0.330), mucoadhesion strength (68.15±0.37-82.24±0.72%) and drug release at 12 h (67-84%). Among the microspheres formulation, an F1 batch of (0.5:1) drug: polymer concentration and at 4% concentration of calcium chloride as a crosslinker was considered best formulation with reduced particle size 32.85±0.774μm, % intro mucoadhesion. 82.24±0.72. In vitro mucoadhesion strength was increased with the increasing crosslinking time from 5 min to 10 min. The fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) study showed no interaction between drug and polymer. X-ray diffraction (XRD) spectrum of microspheres indicates that drug particles are dispersed at the molecular level in the polymer matrices so no indication of the crystalline nature of the drug nature. Scanning electron microscopic (SEM) study showed that microspheres were spherical in shape with a smooth surface. F1 batch shows percentage cumulative drug release 84.07%. In vitro dissolution studies indicates that percent cumulative drug release from microspheres follows zero order kinetics plot which indicates controlled-release drug-delivery for 12 h which leads to control of plasma concentration.Conclusion: The results show that the formulation that contains (0.5:1) drug: polymer ratio, calcium chloride in 4% concentration and crosslinking time 10 min is the best one and can be utilized to formulate risedronate sodium mucoadhesive microspheres to enhance gastric residence time, improved patient compliance and reduction in the frequency of drug administration.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF NOVEL HERBAL FORMULATION (POLYMERIC MICROSPHERES) OF SYZYGIUM CUMINI SEED EXTRACT

2018 ◽  
Vol 10 (5) ◽  
pp. 226
Author(s):  
Ranu Biswas ◽  
Kalyan Kumar Sen
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Xrd Analysis ◽  
Syzygium Cumini ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Polymeric Microspheres ◽  
Herbal Formulation ◽  
Alkaline Dissolution ◽  
The Fourier Transform

Objective: The purpose of the present investigation was to develop and characterize a novel herbal formulation (polymeric microspheres) of Syzygium cumini seed extract.Methods: The extract-loaded microspheres using biological macromolecule ethyl cellulose (EC) was prepared by o/w emulsion solvent evaporation technique using polyvinyl alcohol (PVA) emulsifier. The effect of various process and formulation variables (stirring speed, evaporation time, drug/polymer ratio and organic/aqueous phase ratio) on the properties of microspheres was evaluated.Results: Micromeritic properties indicated good flow properties, and scanning electron microscopy (SEM) confirmed the spherical nature of the prepared microspheres. The particle size and entrapment efficiency were varied between 34.25 to 176.25 µm and 10.51 to 42% depending upon the variables. All the formulations showed minimal drug release in an acidic environment (pH 1.2) confirming the prevention of drug release in the stomach and enteric nature of the polymer. Sustained drug release has been observed in alkaline dissolution media (pH 7.4) after 12 h of drug release study except for formulation F7 which contains a lower concentration of polymer. The fourier transform infrared spectroscopy (FTIR) analysis indicated the compatibility of the extract with the polymer. The absence of extract-polymer interaction was indicated by the differential scanning calorimetry (DSC) thermogram. x-ray diffraction (XRD) analysis revealed the amorphous nature of the extract in the microspheres which in pure form exhibits a crystalline structure.Conclusion: The findings of this present study suggest that microsphere formulation was a promising carrier for novel delivery of herbal drugs.

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