scholarly journals Formulation and Characterization of Modified Release Microspheres of Lornoxicam Using Okra Gum as Natural Polymer and Ethyl Cellulose as Synthetic Polymer

2021 ◽  
pp. 299-326
Author(s):  
Ashwin Kumar Saxena ◽  
Navneet Verma
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Entrapment Efficiency ◽  
Synthetic Polymer ◽  
Fickian Diffusion ◽  
Natural Polymer ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency ◽  
Okra Gum

Objective: The nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most widely used medications in the world because of their demonstrated efficacy in reducing pain and inflammation. The arthritis, pain and inflammation are effectively treated with Lornoxicam, an effective NSAIDs. Because the drug is weakly acidic, it is absorbed easily in the GI tract, and has a short biological half-life of 3 to 5 hours. To meet the objectives of this investigation, we developed a modified release dosage form to provide the delivery of lornoxicam at sustained rate which was designed to prolong its efficacy, reduce dosage frequency, and enhance patient compliance. The present research work was focused on the development of lornoxicam microspheres using natural polymer like okra gum extracted from the pods of Abelmoschus esculentus Linn. and synthetic polymer like ethyl cellulose along with sodium alginate prepared by Ca2+ induced ionic-gelation cross-linking in a complete aqueous environment were successfully formulated. Materials and Method: The microspheres were prepared by using sodium alginate with natural polymer (okra gum) and synthetic polymer (ethyl cellulose) in different ratios by Ca2+ induced ionic-gelation cross-linking. The formulations were optimized on the basis of drug release up to 12 hrs. The physicochemical characteristics of Lornoxicam microspheres such as drug polymer interaction study by Fourier Transform Infrared (FTIR) and further confirmation by Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD). The formulated microspheres were characterized for particle size, percentage drug entrapment efficiency, micromeritic properties, surface morphology, percentage swelling index, in-vitro drug release study and mechanism of drug release. Results and Discussion: The FTIR Spectra revealed that there was no interaction between polymer and Lornoxicam which was further confirmed by DSC and XRD. All the formulated Lornoxicam microspheres were spherical in shape confirmed by SEM. The microspheres exhibited good flow properties and also showed high percentage drug entrapment efficiency. All the batches have excellent flow properties with angle of repose in the range of 25.38° ± 0.04 to 30.41° ± 0.07, carr’s index and hausner’s ratios in the range of 10.40% ± 0.018 to 16.66% ± 0.012 and 1.128 ± 0.09 to 2.225 ± 0.01, respectively. The optical microscopic studies revealed that the mean particle size of all the formulations were found in the range of 819.46 ± 0.07 to 959.88 ± 0.02 μm and percentage of drug entrapment were found to be between 72.35 ± 0.02 to 90.00 ± 0.05. Swelling index of prepared microspheres revealed that with increasing the polymer ratios, there were increase in the swelling of prepared microspheres, showing in the range of 600.76 ± 0.42 to 690.11 ± 0.03% for okra gum microspheres at the end of 9 hr in comparison with ethyl cellulose microspheres which ranges between 179.71 ± 0.07 to 227.73 ± 0.05% at the end of 7 hr. In-vitro drug release of prepared microspheres formulation code LSO4 and LSE4 were found to be 88.654 ± 0.25% and 93.971 ± 0.20% respectively at the end of 12 hr. It was suggested that increase in polymer concentration, the drug release from the prepared microspheres got retarded producing sustained release of lornoxicam. In-vitro drug release data obtained were fitted to various release kinetic models to access the suitable mechanism of drug release. Drug release from lornoxicam-loaded alginate-okra gum microspheres followed a pattern that resembled sustained release (Korsemeyer-Peppas model) (R2 = 0.9925 to 0.9951), and n ≤ 1 indicated anomalous diffusion (non-Fickian), supercase-II transport mechanism LSO4 (n = 1.039) over a period of 12 hour underlying in-vitro drug release. Moreover, zero order model (R2 = 0.9720 to 0.9949) were found closer to the best-fit Korsemeyer - Peppas model. In addition, the drug release from lornoxicam-loaded alginate-ethyl cellulose microspheres also follow Korsemeyer-Peppas model (R2 = 0.9741 to 0.9973) with near to Hixson-Crowell model (R2 = 0.9953 to 0.9985) and n < 1 indicated non-Fickian diffusion or anomalous transport mechanism. Moreover, first order model with non-Fickian diffusion mechanism (R2 = 0.9788 to 0.9918) were found closer to the best-fit Korsemeyer-Peppas model/ Hixson-Crowell model. Conclusion: The present study conclusively demonstrates the feasibility of effectively encapsulating Lornoxicam into natural polymer (okra gum) and synthetic polymer (ethyl cellulose) to form potential sustained drug delivery system. In conclusion, drug release over a period of 12 hrs, could be achieved from these prepared microspheres. A pH-dependent swelling and degradation of the optimized microspheres were also observed, which indicates that these microspheres could potentially be used for intestinal drug delivery.

scholarly journals Design and Development of Brahmi Extract Loaded Nanofibers for Cognitive Disorder and Its Optimization

2019 ◽  
pp. 104-115
Author(s):  
Shete Sanmati D. ◽  
Amane Nikita B. ◽  
Desai Punam S. ◽  
Salunkhe .V. R. ◽  
Magdum C. S.
Keyword(s):  
Mental Health ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Mental Health Disorders ◽  
Synthetic Polymer ◽  
In Vitro Drug Release ◽  
Site Of Action ◽  
Drug Entrapment Efficiency ◽  
Health Disorders

Cognitive disorders (CDs), also known as neurocognitive disorders (NCDs) are a category of mental health disorders that primarily affect cognitive abilities including learning, memory, perception, and problem solving. Global population with depression ranges mostly between 2% and 6% around the world today. Mental health disorders are also attributed to significant number of indirect deaths through suicide and self-harm. The aim of designing a drug delivery system is to enable drug release at a controlled rate over a desired period. nanofibers, with their large specific surface areas, can improve the solubility and dissolution rates of drugs, thereby resulting in fast release of poorly soluble active drugs. Drug release from nanofibers in terms of processing setup and modulate the release kinetics, to achieve site of action with increased plasma half life and resulting increasing residence time of drug in plasma, slowing down rapid renal clearance and helping extended presence of drug at the site of action and also minimize the toxicity of drug. Bacopa monniera an Ayurvedic drug which is mainly used for health practices. Polyvinylpyrrolidone as synthetic polymer was preferably used as a carrier for preparation of nanofibers. Nanofibers mainly prepared by using synthetic polymer because it does not have any toxic effect. Pre-formulation studies were carried out. Experimental design based on trial and error base. Total three batches were prepared using chitosan, cellulose acetate and Polyvinylpyrrolidone.FT-IR Spectroscopy study showed that there was no interaction between drug and polymer. Nanofibers were prepared by using electrospinning method. After preparation of nanofibers were subjected to various evolution parameters includes practical yield, in-vitro drug release, drug entrapment efficiency, SEM,XRD, Zeta Potential, FTIR. The formulations were optimized with respect to In-Vitro drug release and drug entrapment efficiency. Among the all formulations, the Brahmi Extract loaded PVP nanofibers batch F1 containing 300mg of brahmi extract and 600 mg polymer was optimized because this batch showed 97.57% drug release,99.24% drug entrapment efficiency,-26.4mV Zeta potential of the optimized batch which is mainly used to check the stability of the nanofibers formulation. An optimized formulation brahmi extract loaded nanofibers batch F1 is well acceptable, pleasant, palatable and with better compliance.

Formulation and Evaluation of Luliconazole Microsponges Loaded Gel for Topical Delivery

2021 ◽  
pp. 5775-5780
Author(s):  
Farhana Sultan ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Production Yield ◽  
In Vitro Drug Release ◽  
Eudragit Rs ◽  
Diffusion Studies

Microsponge containing Luliconazole (LCZ) with different proportion of drug:polymer (Ethyl cellulose and Eudragit RS 100) were obtained efficiently using Quasi-emulsion solvent diffusion method. Luliconazole is an anti-fungal drug used for the topical delivery. The purpose of the microsponge formulation is to control the release of LCZ drug to the skin through Microsponge Delivery System (MDS) known to be the novel technique which overcome the maximum concentration of active ingredient, frequency doses, and skin irritation. The prepared microsponges were examined using drug content, % production yield, % entrapment efficiency and in-vitro drug release. The formulation were subjected to in-vitro drug release studies for 6 hr in which it was concluded that Ethyl cellulose microsponges formulated by drug:polymer (1:1) and Eudragit RS 100 microsponges formulated by drug:polymer (1:3) showed maximum controlled release i.e., Increase in drug:polymer ratio (1:1 to 1:9) increased the production yield and entrapment efficiency of microsponges using Ethyl cellulose with no significant effect for Eudragit RS 100.Therefore, both formulation F1 and F2 was dispersed in carbopol gel preparation for controlled delivery of LCZ to the skin. Various physical parameters like pH, spreadability, viscosity and in-vitro drug diffusion studies were evaluated for the prepared gel formulations. Microsponge gel formulation i.e., FG1 showed better results for controlled release of 89.40% as compared to FG2 i.e., 92.18% over the period of 12 hrs which is performed in Franz Diffusion Cell. On basis of in-vitro diffusion studies for LCZ gel formulation, microsponges using Ethyl cellulose (FG1) was found to be best for its controlled release of LCZ for 12 hrs and followed zero order kinetics. Hence, formulated LCZ loaded gel have potential to treat fungal infections i.e., tinea pedis, tinea cruris and tinea corporis.

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.

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.

Etoposide-Loaded Microparticles Prepared with Poly (Hydroxybutyrate-Co-Hydroxyvalerate) and Poly(-Caprolactone) Blends: Formulation, Characterization and in vitro Drug Release

1970 ◽  
Vol 1 (3) ◽  
pp. 251-256
Author(s):  
Patel J. K ◽  
Tank H. M
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Evaporation Process ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Drug Entrapment Efficiency ◽  
Solvent Evaporation Process ◽  
Poly Caprolactone

The purpose of this research was to formulate and systematically evaluate etoposide-loaded microparticles. Etoposide microparticles containing poly(hydroxybutyrate-co-hydroxyvalerate) and poly(-caprolactone) were prepared by an emulsion/solvent evaporation process. Microparticles were discrete, spherical and free flowing. The microparticles showed high % of yeild and drug entrapment efficiency. Etoposide-loaded microparticles demonstrated drug sustained releases (up to 200 hours). The drug release mechanism was dependent on the presence of PCL in the microparticles. The release of etoposide caused an increase in the surface area of the microparticles. A Fickian release was determined for the microparticles prepared exclusively with P(HBHV), while non-Fickian release behaviors were found for the P(HBHV)/PCL microparticles.

Preparation and Release Profiles of a Solid Oleoylchitosan Coated Poly(lactic-co-glycolic acid) Nanoparticles

2014 ◽  
Vol 936 ◽  
pp. 717-722
Author(s):  
Yan Yan Li ◽  
Feng Song Liu
Keyword(s):  
Drug Release ◽  
Glycolic Acid ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Release Behavior ◽  
Release Rates ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency ◽  
Model Drug

A solid oleoylchitosan (OCS) coated Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (OCS-coated PLGA NPs) were prepared using the emulsification–evaporation method. The nanoparticles in suspension (TEM) and solid state (SEM) were spherical and very regular and compact. The effects of OCS concentration, PLGA concentration, drug concentration, and release media on drug entrapment efficiency and in vitro drug release behavior were investigated for the release properties using rifampicin (RFP) as a model drug. Both the increase of PLGA concentration and the increase of OCS concentration could decrease the drug release rates. The RFP release rates decreased as the RFP concentration increased. The RFP release rate was sensitive to the pH of the release media.

scholarly journals Preparation and Evaluation of Chitosan Microcapsules of Metronidazole using Tripolyphosphate Cross-linking Method

1970 ◽  
Vol 9 (2) ◽  
pp. 125-130 ◽  
Author(s):  
Akanksha Garud ◽  
Navneet Garud
Keyword(s):  
Drug Release ◽  
Surface Morphology ◽  
Entrapment Efficiency ◽  
Cationic Polymer ◽  
Cross Linking ◽  
In Vitro Drug Release ◽  
Long Duration ◽  
Drug Entrapment Efficiency ◽  
Preparation And Evaluation

Metronidazole microcapsules with a coat consisting of alginate and the natural cationic polymer, chitosan were formulated by using tripolyphosphate cross-linking method and were investigated with a view to develop mucoadhesive microcapsules. The microcapsules were evaluated for their surface morphology, microencapsulation efficiency, in-vitro wash-off test, swelling behavior and in-vitro drug release. The microcapsules formed had rough surface morphology in scanning electron microscopy. The drug entrapment efficiency was found to be in the range 75.2±1.31% and 82.1±0.75%. Chitosan microcapsules displayed a limited amount of swelling which is supposed to be related to the degree of cross-linking with tripolyphosphate. The microcapsules showed better mucoadhesive property at intestinal pH 7.4 than at gastric pH 1.2 in the in-vitro wash-off test. The drug release was found to be slow and extended over long duration of time. Key words: Metronidazole microcapsules; chitosan; mucoadhesion; tripolyphosphate DOI: http://dx.doi.org/10.3329/dujps.v9i2.7897 Dhaka Univ. J. Pharm. Sci. 9(2): 125-130, 2010 (December)

Formulation, optimization, and characterization of amlodipine besylate loaded polymeric nanoparticles

2021 ◽  
Vol 29 (9_suppl) ◽  
pp. S1555-S1568
Author(s):  
Vibha Chourasiya ◽  
Sarvesh Bohrey ◽  
Archna Pandey
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Amlodipine Besylate ◽  
Process Yield ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

The objectives of this work were to formulate and optimize amlodipine besylate loaded polymeric nanoparticles by using factorial design. The emulsion solvent evaporation method was employed successfully to produce the drug loaded polymeric nanoparticles and the optimization was done by the help of the 24 factorial design. The effect of the main preparation variables on the dependent variables such as nanoparticle size and % drug entrapment efficiency was studied for the optimization of the nanoparticles. The characterization of these nanoparticles was done by the different parameters such as interaction between the excipients, size, morphology, zeta potential, % drug entrapment efficiency, % process yield, and in-vitro drug release behavior. FTIR, DLS, TEM, AFM, zeta potential studies, and dialysis bag method were performed for this purpose. The in vitro drug release data were analyzed by different kinetic models to know the release mechanism. The optimized nanoparticles were spherical in shape and showed particle size 91.5 ± 4.3 nm, PDI 0.368 ± 0.014, zeta potential −17.5 mV, % drug entrapment efficiency 74.06 ± 2.1%, and % process yield 78.51 ± 1.8%. The release kinetics studies revealed that drug release from the nanoparticles follow the Korsmeyer–Peppas model.

Formulation and Evaluation of Spray Dried Microspheres of Controlled Release Ramipril

2018 ◽  
Vol 11 (2) ◽  
pp. 4059-4066
Author(s):  
Chetankumar Mutagond ◽  
Vinod M R ◽  
Vijapure V M ◽  
Marapur S C ◽  
R G Patil ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Entrapment Efficiency ◽  
X Ray Diffraction ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency ◽  
Controlled Released ◽  
Spray Dried

The present study sought to develop and evaluate spray-dried microspheres of chitosan and xanthan gum for controlled release of ramipril, a widely used antihypertensive drug. The prepared microspheres were characterized by particle size analysis, scanning electron microscopic studies, differential scanning calorimetric analysis, Fourier transform infrared spectroscopy analysis, X-ray diffraction studies, drug entrapment efficiency, and in-vitro drug release study. The prepared microspheres were spherical in shape and freely flowing. The size of the microspheres was in the range of 25.7 to 47.4 µm and the drug entrapment efficiency was in the range of 74.68% to 90.44%. TheDSC analysis and X-ray diffraction studies indicated that the drug was uniformly dispersed in amorphous state in the microspheres. The in-vitro drug release indicated that the spray-dried microspheres prepared with chitosan alone were not suitable for controlled released delivery of drug as maximum amount of drug was released within 5 hrs. Whereas microspheres prepared by xanthan gum released small amount of drug within 5 hrs and more amount of drug was controlled released that fit the therapeutic needs. Drug release mechanism followed non-Fickian transport. These suggest the formulation potential of chitosan and xanthan gum for spray-dried microspheres for controlled release of ramipril

scholarly journals Formulation and evaluation of lansoprazole loaded enteric coated microspheres

2020 ◽  
Vol 1 (4) ◽  
pp. 124-130
Author(s):  
SK. Haneesha ◽  
M. Venkataramana ◽  
N. Ramarao
Keyword(s):  
Drug Release ◽  
Intestinal Absorption ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Film Coating ◽  
In Vitro Drug Release ◽  
Evaporation Technique ◽  
Drug Entrapment Efficiency ◽  
Enteric Coated

The research focuses on the development of multiparticulate delivery system for acid-labile Lansoprazole to prevent its degradation in the acidic environment of the stomach and enhance its bioavailability via intestinal absorption. This problem can be solved by enteric coating. In this project, cellulose acetate phthalate a polymer usually utilized for gastrointestinal film coating of tablets, was used to prepare enteric microspheres of lansoprazole with solvent evaporation technique in various formulations such as F1, F2, F3, F4, F5 with drug: polymer ratios of 1:1, 1:2, 1:3, 1:4, 1:5 respectively. FTIR study indicated compatibility between drug and polymer. Increase in concentration of polymer increased spheriocity and mean diameter of the microspheres. The drug entrapment efficiency was in the range of 72.23% to 88.64%. SEM revealed that microspheres were found spherical and porous. In-vitro study proves that drug release slowly increases as the pH of the medium increased and prevents degradation of drug in acidic pH. In-vitro drug release was found to be 92.80%, 94.55%, 92.72%, 96.34%, 98.65% in all 5 formulations. All 5 formulations showed gastric resistance around 80-90%. So it is concluded that the developed enteric coated microspheres of Lansoprazole prevented drug release in the stomach which would lead to significant improvement in its bioavailability through enhanced intestinal absorption.

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