Effect of Various Electrolytes on Theophylline Loaded Sodium Alginate Beads Prepared by Ionic Cross Linking Technique

The purpose of t h e present research work was to prepare alginate beads containing water soluble drug theophylline using ionic cross linking technique, with electrolyte type and concentration as variables. In this study, the beads were characterized and evaluated in respect of their surface morphology, swelling index and in vitro kinetics. The comparative study among the three polyvalent cationic cross linking agents CaCl2 , BaCl2 and Al2 (SO4)3 were investigated based on their cationic charges. Divalent cation, Ca2+ and Ba2+ containing beads showed simultaneous decrease in drug release with increasing electrolyte amount. In case of Al3+ -alginate beads, the delay in release was due to the ability of Al3+ to form three dimensional bonding structure with the sodium alginate inside the beads. As a result, swelling of beads is delayed leading to slow disintegration. Scanning electron microscope (SEM) photomicrographs revealed that with the increase in the electrolyte concentration the density of the cross link is also increased. When the electrolyte concentration is 5 % then the beads surface is rough and rod shape drug is visible. But when the electrolyte concentration is increased from 10 % to 15 % the surface is comparatively smoother and both the swelling property and in vitro drug release are decreased. Most of the formulations followed Higuchi drug release model. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14578 Dhaka Univ. J. Pharm. Sci. 11(2): 181-189, 2012 (December)

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Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.5.7 ◽

2016 ◽

Vol 9 (5) ◽

pp. 3494-3501

Author(s):

Bipul Nath ◽

Santimoni Saikia

Keyword(s):

Drug Release ◽

Sodium Alginate ◽

Alginate Beads ◽

In Vitro Drug Release ◽

Dsc Studies ◽

Ft Ir ◽

Lag Period ◽

Pulsatile Delivery ◽

Ca Alginate

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.

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DESIGN AND EVALUATION OF CONTROLLED-RELEASE OCULAR INSERTS OF BRIMONIDINE-TARTRATE AND TIMOLOL MALEATE

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i1.15199 ◽

2016 ◽

Vol 9 (1) ◽

pp. 79 ◽

Cited By ~ 2

Author(s):

Preethi G. B. ◽

Prashanth Kunal

Keyword(s):

Controlled Release ◽

Drug Release ◽

Sodium Alginate ◽

Calcium Chloride ◽

Release Kinetics ◽

Water Soluble ◽

Moisture Loss ◽

Timolol Maleate ◽

Brimonidine Tartrate

Objective: The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.Methods: Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and in vitro release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.Results: It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. Conclusion: It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, in vitro drug release and stability.

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DESIGN, DEVELOPMENT, AND CHARACTERIZATION OF OROMUCOSAL WAFER OF TRAMADOL HYDROCHLORIDE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i8.25709 ◽

2018 ◽

Vol 11 (8) ◽

pp. 116

Author(s):

Rita N Wadetwar ◽

Tejaswini Charde

Keyword(s):

Drug Release ◽

Biodegradable Polymer ◽

Research Work ◽

Water Soluble ◽

Content Uniformity ◽

Onset Of Action ◽

Water Soluble Polymer ◽

Surface Ph ◽

Folding Endurance

Objective: The objective of the present work was the preparation of fast-dissolving film of tramadol HCl (TMH) using water-soluble polymer, to achieve faster onset of action, to improve patient compliance, ease of dosing, and bypass the first-pass metabolism. Methods: TMH oromucosal wafers were prepared using pullulan as natural, biodegradable polymer, and propylene glycol as plasticizer by solvent casting method. Formulation batches were prepared using 32 full-factorial designs. The prepared TMH oromucosal wafers were characterized for morphology, uniformity of weight, drug content, folding endurance, in vitro disintegration time (DT), % moisture content, surface pH, in vitro % drug release, ex vivo permeation studies, compatibility studies (differential scanning calorimetry, Fourier transform infrared spectroscopy, and X-ray diffraction), and stability studies.Results: Optimized batch of mouth-dissolving film of TMH containing pullulan as polymer showed 98.67±0.11% drug release at 6 min. It showed better folding endurance 88 No. of folds, in vitro DT 5.11 s, surface pH 6.84±0.12 pH, thickness 0.17±0.11 mm, and percentage content uniformity 98.45±0.48%. Stability studies carried out for the best formulation FDF5 revealed that the formulation was stable.Conclusion: The results obtained in this research work clearly indicated a promising potential of fast-dissolving oral films using natural biodegradable polymer, pullulan which gave rapid drug delivery and rapid onset of action of centrally acting drug, TMH for patients suffering from pain.

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FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5.1943 ◽

2018 ◽

Vol 8 (5) ◽

pp. 465-474

Author(s):

S PADMA PRIYA ◽

AN Rajalakshmi ◽

P Ilaveni

Keyword(s):

Drug Release ◽

Sustained Release ◽

Sodium Alginate ◽

Release Kinetics ◽

Drug Loading ◽

Research Work ◽

Entrapment Efficiency ◽

Polyvinyl Pyrrolidone ◽

Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods: Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine formulations were formulated and evaluated for possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

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Preparation and preclinical evaluation of aceclofenac loaded pectinate mucoadhesive microspheres

Drugs and Therapy Studies ◽

10.4081/dts.2012.e8 ◽

2012 ◽

Vol 2 (1) ◽

pp. 8 ◽

Cited By ~ 1

Author(s):

Santanu Chakraborty ◽

Priyanka Nayak ◽

Bala Murali Krishna ◽

Madhusmruti Khandai ◽

Ashoke Kumar Ghosh

Keyword(s):

Particle Size ◽

Drug Release ◽

Polymer Concentration ◽

Research Work ◽

In Vivo Studies ◽

Systemic Absorption ◽

Cross Linking ◽

Significant Difference

The aim of the present research work was to fabricate aceclofenac loaded pectinate microspheres by ionic gelation method and evaluate the effect of different cross-linking agents and polymer concentration on particle size, encapsulation efficacy and drug release behavior. It was also investigated that whether this pectinate dosage form was able to target the drug release in intestinal region and prevent the different side effect associated with the drug in stomach or not. It was observed that particle size, encapsulation efficacy and in vitro drug release were largely depended on polymer concentration and cross-linking agents. It was also observed that pectinate microspheres showed excellent pH depended mucoadhesive properties and they were able to restrict the drug release in stomach. In vitro drug release study showed that alminium-pectinate microspheres have more sustaining property as compared to barium-pectinate microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t50% values among all the formulations with same cross-linking agent. In vivo studies revealed that the anti inflammatory and analgesic effects induced by pectinate microspheres were significantly high and prolonged as compared to pure drug. So, pectinate microspheres can be an excellent carrier for targeting the delivery of aceclofenac as well as help in improving the patient compliance by prolonging the systemic absorption.

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Formulation and optimization of water soluble granules of Withania Somnifera

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v11i6.5142 ◽

2021 ◽

Vol 11 (6) ◽

pp. 26-30

Author(s):

Dilip Kumar Tiwari ◽

Kaushelendra Mishra ◽

Neelima Mishra ◽

Neeraj Upmanyu

Keyword(s):

Drug Release ◽

Potential Benefit ◽

Withania Somnifera ◽

Research Work ◽

Herbal Medicines ◽

Water Extract ◽

Water Soluble ◽

Nootropic Activity ◽

In Vitro Drug Release

Herbal medicines have great demand in the treatment of various kinds of illness. Ayurvedic system of medicine has consisted of many herbal sources in which ashwagandha one of them which are the very popular herbal sources. Many literature surveys suggest that ashwagandha is used as an immunomodulator, tranquilizer, antioxidant, antidiabetic, and nootropic activity. Present research work explored the potential benefit of ashwagandha by designing suitable granules of its water extract. Further, it is characterized by various parameters and In-vitro drug release Keywords: Immunomodulator, Tranquilizers Ayurvedic, Ashwagandha, Granules

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Effect of Various Excipients on Theophylline-loaded Alginate Beads Prepared by Ionic Cross Linking Technique

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v9i1.7425 ◽

1970 ◽

Vol 9 (1) ◽

pp. 15-22 ◽

Cited By ~ 1

Author(s):

Sheikh Tasnim Jahan ◽

Sams Mohammad Anwar Sadat ◽

Md Saiful Islam ◽

Reza-ul Jalil ◽

Jakir Ahmed Chowdhury

Keyword(s):

Polyethylene Glycol ◽

Drug Release ◽

Sodium Alginate ◽

Methyl Cellulose ◽

Alginate Beads ◽

Cross Linking ◽

Carboxy Methyl Cellulose ◽

Polyethylene Glycol 4000 ◽

Sodium Starch Glycolate ◽

Carboxy Methyl

Theophylline loaded sodium alginate beads were prepared by ionic cross linking technique using calcium chloride (CaCl2) as cross linking agents. The purpose of this work was to prepare sodium alginate beads as a device for the extended release of theophylline. Different excipients like sodium carboxy methyl cellulose, polyethylene glycol 4000, hydroxy propyl methyl cellulose, sodium starch glycolate, Eudragit L 100 and sodium lauryl sulphate were used to fabricate theophylline-alginate beads and their effect on drug release were investigated. In this study, the beads were characterized and evaluated in respect to their surface morphology, swelling index (SI) and in-vitro release characteristics. Beads were prepared by dropping a hot aqueous theophylline-alginate or theophylline-alginate-excipient solution into electrolyte solution. Alginate cross linked with electrolytes and beads were formed with entrapped drug. Beads were collected by decanting the solution and dried at room temperature. Surface of beads with various excipients revealed that smooth, dense and closely packed drug-polymer bonding was obtained when the excipients were changed. Beads in F 1 contain Eudragit L 100 that swelled highest at 3 hours with SI of 10.74 %. Sodium starch glycolate beads (F 4) swelled high up to 9.93 % at 2 hours. Dissolution studies were carried out in 900 ml of distilled water for 8 hours. Most of the formulations were fitted to Higuchi model. The drug release rate are shown in decreasing order: Eudragit L 100>Sodium carboxy methyl cellulose> Sodium lauryl sulphate> Sodium starch glycolate>Hydroxy propyl methylcellulose 5 cps>Polyethylene glycol 4000. The use of Eudragit L 100 was found to be promising because it released about 69 % of theophylline within 8 hours. It was found that among the hydrophilic polymers used, Sodium carboxy methyl cellulose showed 49 % theophylline release within 8 hours. The lowest amount of drug release was found with HPMC 5 cps and PEG 4000 which was about 26 % of drug release. Key words: Theophylline; ionic cross-linking technique; sodium alginate beads; swelling index; release kinetics. DOI: 10.3329/dujps.v9i1.7425 Dhaka Univ. J. Pharm. Sci. 9(1): 15-22 2010 (June)

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TRANSDERMAL DELIVERY OF AN EFFECTIVE NONSTEROIDAL ANTI-INFLAMMATORY DRUGS FOR PAIN MANAGEMENT IN ARTHRITIS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2020.v13i7.37058 ◽

2020 ◽

pp. 41-47

Author(s):

MANJULA D ◽

ABHISHEK RAJ ◽

JOSEPHINE LENO JENITA J ◽

SHANAZ BANU

Keyword(s):

Drug Release ◽

Sodium Alginate ◽

Guar Gum ◽

Research Work ◽

Albino Rats ◽

Drug Content ◽

In Vitro Permeation ◽

Permeation Studies ◽

Anti Inflammatory

Objective: The current research work has been carried out with the aim to develop a transdermal gel formulation of fenoprofen (a nonsteroidal anti-inflammatory drug used to treat pain associated in arthritis) which would overcome the gastrointestinal-related problems associated with oral administration of the drug. The present study aims at formulating transdermal gels using different concentrations of Carbopol, hydroxypropyl methylcellulose (HPMC), sodium alginate, and guar gum. Methods: The formulated gels were subjected for various evaluation tests such as clarity, homogeneity, viscosity, drug content, pH, spreadability, and in vitro permeation studies. Drug–polymer interaction was studied by Fourier transmission infrared (FTIR) and differential scanning calorimetry (DSC). The in vitro permeation studies were performed in phosphate buffer 7.4 using Franz diffusion cell. Results: The FT-IR and DSC studies showed no chemical interaction between drug and polymers used. All the formulated gels showed acceptable physical properties with respect to clarity, homogeneity, viscosity, drug content, pH, and spreadability. Among all the gel formulations, Carbopol gels containing fenoprofen showed good drug release compared to HPMC, sodium alginate, and guar gum. Optimized formulation was further subjected to kinetic studies which showed Higuchi model of drug release. The same formulation showed significant anti-inflammatory and analgesic activity, tested in Wistar albino rats. No signs of erythema, edema, flushing, and papules were observed when skin irritation test was performed. Stability studies under accelerated condition showed satisfactory results for the optimized formulation. Conclusions: Thus, it was concluded from the results that the optimized formulation showed controlled and slow drug delivery. Animal studies were significant at p<0.05 and 0.001. The selected formulation was stable at various ambient temperatures.

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Formulation and Evaluation of Pseudoephedrine Hydrochloride Loaded Alginate Microbeads

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i3.4094 ◽

2020 ◽

Vol 10 (3) ◽

pp. 137-141

Author(s):

Rashmi Dahima

Keyword(s):

Drug Release ◽

Sodium Alginate ◽

Cost Effective ◽

Alginate Beads ◽

Controlled Delivery ◽

In Vitro Drug Release ◽

Release Studies ◽

Multiple Unit ◽

Effective Carrier

Multiple unit dosage forms such as microbeads have increased acceptance because of added even spreading of the drug in the gastrointestinal tract, unvarying drug absorption, abridged local irritation and removal of undesirable intestinal retaining of polymeric material, when compared to non-disintegrating single unit dosage form. The purpose of the presented research is to develop microbeads of pseudoephedrine hydrochloride utilizing sodium alginate as the hydrophilic carrier in combination with HPMC as drug release modifier to lessen the dosing frequency and thereby advance the patient compliance. The microbeads were formulated by varying concentrations of HPMC and calcium chloride. The optimum formulation was chosen based upon in vitro drug release studies and further evaluated. The compatibility of drug-polymer was studied using FTIR analysis. The prepared formulation underwent evaluation for various parameters like drug entrapment, microbeads size, swelling index, mucoadhesive property and stability. No significant drug-polymer interactions were observed in compatibility studies and the formulation was found to be stable on 45 days storage. The formulations exhibited an extended drug release pattern which was the ultimate aim of the study. The microbeads represented good yield, high drug entrapment, low microbeads size and appropriate swelling property. The in vitro wash-off test indicated that the sodium alginate microbeads represent decent mucoadhesive properties. Henceforth, the formulated HPMC coated sodium alginate beads can be utilized as a substitute and cost-effective carrier for the oral controlled delivery of pseudoephedrine hydrochloride. Keywords: microbeads, pseudoephedrine hydrochloride, sodium alginate, drug release

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Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities

Marine Drugs ◽

10.3390/md19080467 ◽

2021 ◽

Vol 19 (8) ◽

pp. 467

Author(s):

Mohammed F. Aldawsari ◽

Mohammed Muqtader Ahmed ◽

Farhat Fatima ◽

Md. Khalid Anwer ◽

Prakash Katakam ◽

...

Keyword(s):

Antioxidant Activity ◽

Particle Size ◽

Drug Release ◽

Drug Loading ◽

Polymer Concentration ◽

Crosslinking Agent ◽

Alginate Beads ◽

Water Soluble ◽

Ca Alginate

The objective of this work was to develop sustained-release Ca-alginate beads of apigenin using sodium alginate, a natural polysaccharide. Six batches were prepared by applying the ionotropic gelation technique, wherein calcium chloride was used as a crosslinking agent. The beads were evaluated for particle size, drug loading, percentage yield, and in vitro drug release. Particle size was found to decrease, and drug entrapment efficiency was enhanced with an increase in the polymer concentration. The dissolution study showed sustained drug release from the apigenin-loaded alginate beads with an increase in the polymer proportion. Based on the dissolution profiles, BD6 formulation was optimized and characterized for FTIR, DSC, XRD, and SEM, results of which indicated successful development of apigenin-loaded Ca alginate beads. MTT assay demonstrated a potential anticancer effect against the breast cancer MCF-7 cell lines. The antimicrobial activity exhibited effective inhibition in the bacterial and fungal growth rate. The DPPH measurement revealed that the formulation had substantial antioxidant activity, with EC50 value slightly lowered compared to pure apigenin. A stability study demonstrated that the BD6 was stable with similar (f2) drug release profiles in harsh condition. In conclusion, alginate-based beads could be used for sustaining the drug release of poorly water-soluble apigenin while also improving in vitro antitumor, antimicrobial, and antioxidant activity.

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