FORMULATION AND IN VITRO EVALUATION OF CHITOSAN FILMS CONTAINING LINEZOLID FOR THE TREATMENT OF PERIODONTITIS

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (07) ◽  
pp. 53-58
Author(s):  
Sanjana A. ◽  
Mohammed Gulzar Ahmed ◽  
Jaswanth Gowda B. H. ◽  
Keyword(s):  
Tensile Strength ◽  
Acetic Acid Solution ◽  
In Vitro Release ◽  
Periodontal Pocket ◽  
Release Kinetic ◽  
Burst Release ◽  
Stability Studies ◽  
Weight Variation ◽  
Folding Endurance

The study was aimed to formulate a dental film containing linezolid, a broad spectrum antimicrobial agent which could be easily placed into the periodontal pocket and be capable of delivering therapeutic concentrations of drug for prolonged periods and also reducing the side effects. In the present investigation, chitosan strips containing linezolid in three different concentrations (10, 20, and 30 %w/w with respect to the weight of polymer) were prepared by the solvent casting method, by using 1 %V/V acetic acid solution. The prepared formulations were evaluated for various properties such as weight variation, thickness, folding endurance, moisture loss, tensile strength, in vitro release, release kinetic study and stability studies. The weight variation and thickness were found to be in the range of (0.99-1.58 mg) and (0.92-1.76 mm), the moisture content, folding endurance was found to be maximum for the plain film and minimum for the drug containing formulation. The tensile strength was found to be in the range of (2.44-1.43 kg/ mm2 ) for the formulation. The dissolution studies showed a burst release initially followed by a progressive fall in the release of the drug (91.15 - 95.87 %) and the release kinetics followed the zero-order pattern. The short term stability studies were conducted and there were no significant changes observed. Hence, low dose, site-specific linezolid film is a potential tool for the treatment of periodontitis.

scholarly journals SODIUM CROMOGLYCATE MUCOADHESIVE BUCCAL PATCHES: DESIGN, FABRICATION, IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 10 (2) ◽  
pp. 76 ◽  
Author(s):  
Shereen Ahmed Sabry
Keyword(s):  
Tensile Strength ◽  
Sodium Cromoglycate ◽  
Residence Time ◽  
In Vitro Release ◽  
Moisture Uptake ◽  
Drug Content ◽  
Weight Variation ◽  
Folding Endurance

Objective: The purpose of this study was to design and formulate mucoadhesive buccal patches of sodium cromoglycate (SCG) as an alternative way to overcome its poor oral absorption and short half-life.Methods: Mucoadhesive patches were prepared by solvent casting technique using cellulose acetate butyrate (CAB) alone or in combination with mucoadhesive polymers like SCMC (sodium carboxymethyl cellulose), HPMC 100M (hydroxyl propyl methyl cellulose) and Cbp934P (carbopol) in different concentrations. The successful patches were evaluated for thickness, weight variation, folding endurance, tensile strength, drug content, surface pH, moisture uptake, swelling percentage, mucoadhesion strength, residence time, in vitro release study, ex vivo permeation and in vivo pharmacokinetic studies.Results: The thickness of all prepared patches ranged from 0.210±0.006 to0.355±0.012, folding endurance was more than 300, weight variation did not exceed 0.179±0.015, tensile strength and % elongation ranged from 6.4±0.018 to 13.1±0.024, and from 30.4±0.88 to 53.4±0.78respectively. The swelling percentage after one hour was from 20.8±0.99 to 53.2±1.5. pH of all prepared patches did not exceed 6.8, the drug content was about 99 to 101%, moisture uptake did not exceed 10%. Mucoadhesion strength and residence time ranged from 17.2±0.14 to 51.2±0.26, and from 3.35±0.25 to 7.45±0.28 respectively. The cumulative release percentage of SCG was in the following descending order CAB>CAB with Cbp934P>CAB with HPMC>CAB with SCMC. The optimized patch (F9) decreased the Cmax and increased Tmax compared to the parenteral solution.Conclusion: It can be concluded that mucoadhesive buccal patch is a promising dosage form to prolong the release of SCG and enhance its poor oral bioavailability.

scholarly journals Design and evaluation of Pulsatile drug delivery of Losartan Potassium

2014 ◽  
Vol 12 (2) ◽  
pp. 119-123
Author(s):  
MS Ashwini ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
In Vitro Release ◽  
Losartan Potassium ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Release Studies ◽  
The Stability ◽  
Vitro Release

The study was designed for the investigation of pulsatile device to achieve time or site specific release of Losartan potassium based on chronopharmaceutical considerations. The basic design involves the preparation of cross linked hard gelatin capsules by using formaldehyde, then the drug diluent mixture were prepared and loaded in, which was separated by using hydrogel plugs of different polymers of different viscosities. Prepared formulations were subjected to evaluation of various parameters like weight variation, percentage drug content, in vitro drug release and stability studies. Weight variation and percentage drug content results showed that they were within the limits of official standards. The in-vitro release studies revealed that the capsules plugged with polymer HPMC showed better pulsatile or sustained release property as compared to the other formulations. The stability studies were carried out for all the formulations and formulations F1 & F2 were found to be stable. Dhaka Univ. J. Pharm. Sci. 12(2): 119-123, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17610

scholarly journals Formulation and evaluation of chitosan films containing sparfloxacin for the treatment of periodontitis

2019 ◽  
Vol 9 (1) ◽  
pp. 38-45 ◽  
Author(s):  
Santoshi Naik ◽  
Prasiddhi Raikar ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Periodontal Pocket ◽  
Content Uniformity ◽  
Burst Release ◽  
In Vitro Antibacterial Activity ◽  
Chitosan Films

In the present study an attempt has been made to formulate and evaluate a sustained release periodontal film of Sparfloxacin with biodegradable, cost effective polymer Chitosan. The objective of the study was to formulate intra-pocket periodontal films, which could be easily placed into the periodontal pocket, and thus be capable of delivering therapeutic concentrations of drug. Sparfloxacin is an antibiotic, showing wide spectrum antibacterial activity against a number of periodontal pathogens. Hence Sparfloxacin is selected as model for site specific delivery, i.e., into periodontal pocket for the treatment of periodontitis. In the present investigation Chitosan films containing Sparfloxacin were prepared by solution casting method using acetic acid. The copolymers HPMC K4M, Sodium CMC and Eudragit RL 100 in the concentrations of 10%, 20% and 30% w/w of Chitosan were added into the polymeric solution. Propylene glycol was used as plasticizer. FT-IR and UV spectroscopic methods revealed no interaction between Sparfloxacin and polymers. The drug loaded films were evaluated for their thickness, weight variation, content uniformity, tensile strength, percent elongation, percentage moisture loss, surface pH, folding endurance, in- vitro drug release studies, in - vitro antibacterial activity and stability studies. Periodontal films showed initial burst release of drug on 1st day and then the release was sustained for a period of 8 days. In – vitro antibacterial activity was carried out on staphylococcus aureus and the antibacterial activity was retained for 96 hours. In - vitro release from periodontal films was fit to kinetic models to reveal drug release kinetics. Keywords: Periodontitis, Sparfloxacin, Bio-adhesive polymers.

scholarly journals Development, characterization, in vitro and ex vivo evaluation of antiemetic transdermal patches of ondansetron hydrochloride and dexamethasone

2021 ◽  
Vol 14 (3) ◽  
pp. 067-078
Author(s):  
Kailash Sahu ◽  
Saman Pathan ◽  
Kapil Khatri ◽  
Neeraj Upmanyu ◽  
Satish Shilpi
Keyword(s):  
Tensile Strength ◽  
Moisture Content ◽  
In Vitro Release ◽  
Nausea And Vomiting ◽  
Moisture Uptake ◽  
Drug Content ◽  
Transdermal Patches ◽  
Ondansetron Hydrochloride ◽  
Folding Endurance

The idea of delivering drugs through skin is old, as the use is reported back in 16th century B.C. The husk of the castor oil plant in water was placed on an aching head. Today the transdermal drug delivery is well accepted for delivering drugs to the systemic circulation. The aim of this study was to design a compound transdermal patches containing ondansetrone HCL and dexamethasone for the treatment of nausea and vomiting in case of chemotherapy and regular symptom of nausea and vomiting. In the present work, an attempt has been made to develop a matrix-type transdermal therapeutic system comprising of Ondansetron-HCl and Dexamethasone in different ratios of hydrophilic and hydrophobic polymeric combinations with 15% w/v plasticizer and 5% w/v penetration enhancer were mixed with the polymer solution polymer were using solvent evaporation technique. The patches were further subjected to various characterization studies for prepared transdermal patches along with the thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, In vitro drug permeation study on Franz diffusion cells. Obtained results showed no physical-chemical incompatibility between drugs and polymers. On the basis of results obtained from, tensile strength (18±0.16), folding endurance (126 ± 1 to 68 ± 2), % moisture content (2.9±0.4), % moisture uptake, % drug content (92.41 to 98.9 %), TPEC (Transdermal Patches of Ethyl Cellulose) was selected as optimized formulation. In vitro release of the selected batch, TPEC-1 followed by zero-order and formulation showed 62.69 % drug diffusion within 10 hours. Conclusively, the patches were considered to deliver drugs safely through the skin for a longer period often.

scholarly journals Preparation and Evaluation of Metronidazole-Loaded Pectin Films for Potentially Targeting a Microbial Infection Associated with Periodontal Disease

Polymers ◽  
2018 ◽  
Vol 10 (9) ◽  
pp. 1021 ◽  
Author(s):  
Taepin Junmahasathien ◽  
Pattaraporn Panraksa ◽  
Paytaai Protiarn ◽  
Doosadee Hormdee ◽  
Rajda Noisombut ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Periodontal Disease ◽  
In Vitro Release ◽  
Oral Disease ◽  
Periodontal Pocket ◽  
Diffusion Method ◽  
Burst Release ◽  
Swelling Properties ◽  
Vitro Release

The objective of this study was to develop the metronidazole loaded high and low methoxyl pectin films (HM-G-MZ and LM-G-MZ) for the treatment of periodontal disease. The films were prepared by pectin 3% w/v, glycerin 40% w/v, and metronidazole 5% w/v. The developed films were characterized by scanning electron microscope and evaluated for thickness, weight variation, and elasticity. The developed films showing optimal mechanical properties were selected to evaluate radial swelling properties, in vitro release of metronidazole and the antimicrobial activity against Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans by the disc diffusion method. The results demonstrated that LM-MZ and HM-G-MZ films were colorless and yellowish color, respectively, with the film thickness around 0.36–0.38 mm. Furthermore, both films exhibited good elasticity with low puncture strength (1.63 ± 0.37 and 0.84 ± 0.03 N/mm2, respectively) and also showed slight increase in radial swelling, so that they could be easily inserted and fitted into the periodontal pocket during a clinical use. However, HM-G-MZ showed a decrease in radial swelling after 1 h due to the film erosion. The in vitro release study of LM-G-MZ showed a burst release that was initially followed by a slow release rate profile, capable to maintain the therapeutic level in periodontal pocket for seven days, whereas HM-G-MZ showed an immediate release profile. The cumulative percentage of metronidazole release from HM-G-MZ was less than LM-G-MZ during the first 5 min as metronidazole was in a crystalline form inside HM-G-MZ film. For antimicrobial activity test, both films showed the inhibitory effect against P. gingivalis and A. actinomycetemcomitans, and there was no difference in the inhibition zone between LM-G-MZ and HM-G-MZ. The present study showed, for the first time, that low methoxyl pectin film containing glycerin and metronidazole could be potentially considered as a promising clinical tool for the drug delivery via intra-periodontal pocket to target an oral disease that is associated with polymicrobial infection.

Tamarind Seed Polysaccharide Mouth Dissolving films for rapid drug Release in the treatment of Hypertension: In vitro Evaluation

2021 ◽  
pp. 2771-2773
Author(s):  
Pamula Reddy Bhavanam ◽  
Shaik Abdul Rahaman ◽  
M Mohan Varma
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
In Vitro Drug Release ◽  
Tamarind Seed ◽  
Weight Variation ◽  
Folding Endurance ◽  
Vitro Release

Tamarind seed polysaccharide (TSP) micro sized mouth dissolving films were prepared to release the Amlodipine besylate drug for hypertension. TSP mouth dissolving films were prepared by solvent evaporation method which was further examined under in vitro studies. In vitro antimicrobial activities for all the mouth dissolving films were conducted by diffusion method. Form the in vitro release profile, the AML-TSP was completely showed rapid release of drug up to 98.1% than the thin films of other formulations respectively in the period of time of 10 min. The prepared AML-TSP mouth dissolving films were evaluated for drug content, weight variation, thickness, pH, folding endurance, In vitro drug release and stability studies. AML8 showed the highest drug release at the 10 min time point. The AML8 mouth dissolving film with higher amount of superdisintegrant CCS and SSG showed fastest onset of drug release.

scholarly journals DESIGN AND EVALUATION OF BUCCAL PATCHES CONTAINING COMBINATION OF HYDROCHLOROTHIAZIDE AND ATENOLOL

2018 ◽  
Vol 10 (2) ◽  
pp. 105
Author(s):  
Ashutosh Roda ◽  
Prabhakara Prabhu ◽  
Akhilesh Dubey
Keyword(s):  
Tensile Strength ◽  
Sustained Release ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Content Uniformity ◽  
Casting Technique ◽  
Weight Variation

Objective: Buccal patch is a non-dissolving thin matrix modified release dosage form which was developed to administer into the unconscious and less co-operative patients.Methods: The mucoadhesive buccal patches of hydrochlorothiazide (HCZ) and atenolol (ATN) were prepared by solvent casting technique using various concentrations of sodium alginate, hydroxyl propyl methyl cellulose, carbopol 934P and sodium carboxy methyl cellulose polymer and polyvinyl alcohol as a backing layer. The formulated patches were evaluated for their physicochemical parameters like thickness, weight variation, surface pH, content uniformity, folding endurance, swelling percentage studies and tensile strength, in vitro and ex vivo drug permeation. Results: The infra-red (IR) spectra showed no interaction between drug and polymer. Physicochemical characteristics of all the samples were found to be satisfactory and well within the range. Swelling of the films were increased with the increasing content of the polymers and it was found that swelling front erosion was comparably slower in the formulations with the carbopol 934 and HPMC. This is probably due to their marked viscous properties and therefore formulation provided sustained release of the drug. The percentage drug content of all the formulations were found to be in the range of 97-99 %. Among the patches, FC (Carbopol 934 and HPMC) patches were considered satisfactory for maintaining the in vitro residence in the oral cavity for almost 8h. Formulations FD (with CP and NaCMC) and FC showed high tensile strength and % E/B which is an indication of the strength and elasticity of the patch. The films were exhibited sustained release for more than 6 h which was confirmed by the in vitro release data and kinetic data reveals the combination of diffusion and erosion mechanism. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation FC.Conclusion: The formulation of HCZ and ATN mucoadhesive buccal patch was found to be satisfactory and reasonable.

scholarly journals FORMULATION AND CHARACTERIZATION OF PERIODONTAL FILMS CONTAINING AZITHROMYCIN AND SERRATIOPEPTIDASE

2018 ◽  
Vol 11 (5) ◽  
pp. 205
Author(s):  
Soniya Rani ◽  
Nardev Singh
Keyword(s):  
Moisture Absorption ◽  
Hydroxypropyl Methylcellulose ◽  
Release Profile ◽  
Moisture Loss ◽  
Periodontal Pocket ◽  
Enzyme Release ◽  
Weight Variation ◽  
Folding Endurance

Objective: The objective of the present work was to formulate and evaluate periodontal film, which could be capable of delivering therapeutic concentration of azithromycin and serratiopeptidase for a prolonged period of time and could be easily placed into the periodontal pocket. Methods: The films were prepared by solvent casting method using combinations of ethyl cellulose, hydroxypropyl methylcellulose K4M, hydroxypropyl methylcellulose 50 cps, eudragit L-100, and Chitosan in different ratios using dibutyl phthalate as plasticizer. The periodontal films were evaluated for weight variation, thickness, percentage moisture absorption, percentage moisture loss, folding endurance, percentage swelling index, percentage elongation, and in vitro percentage cumulative drug-enzyme release profile. Results: Formulation F12 was found to be a good periodontal film. Hence, it was considered as an optimized formulation. In vitro drug-enzyme release rate studies using keshary-chien diffusion cell showed maximum drug release in F12 formulation (95.92% for azithromycin and 94.20% for serratiopeptidase at the end of 24 h) compared to other formulations. Conclusion: The optimized formulation F12 showed the best drug-enzyme release profile among the others for the preparation of periodontal film. There is a scope for the further study and development of the azithromycin and serratiopeptidase periodontal films.

scholarly journals A IONTOPHORETIC DELIVERY OF TRANSDERMAL PATCHES CONTAINING ROPIVACAINE: SUSTAINING THE ANESTHETIC EFFECT IN CHILDREN.

2019 ◽  
Author(s):  
Tao Yu ◽  
Shengjie Zhang ◽  
Xu Cao ◽  
Chengyao Liu
Keyword(s):  
Tensile Strength ◽  
Age Groups ◽  
In Vitro Release ◽  
Average Weight ◽  
Physical Parameters ◽  
Transdermal Patch ◽  
Reverse Electrodialysis ◽  
Anesthetic Effect ◽  
Folding Endurance

The present clinical trial investigates the sustaining anesthetic effect of Ropivacaine when administered as epidural injection followed by transdermal patch with and without Reverse electrodialysis (RED) system in order to maintain anesthesia in children. It also focuses on rate of release of drug in-vitro when administered with RED system. The transdermal patch of Ropivacaine was prepared using evaporation technique enclosing 25 mg of Local anesthetic Ropivacaine. Thus prepared patches were evaluated for physical parameters like folding endurance, tensile strength, in vitro drug release etc. The thicknesses of the patches were in the range of 0.02 ±0.006 to 0.04 ± 0.007 mm with 95.79 ±1.85 to 97.45±0.07 % drug content. The average weight and tensile strength was found to be 0.15±0.2 to 0.17±0.18 gm and 0.42±0.006 to 0.58±0.002 kg/cm2. The folding endurance of the patches was in range of 155.21 ±0.2 to 167± 0.29 and content of moisture was 1.43±0.23 % to 2.97±0.23 %. The formulation shows In - vitro release in Phosphate buffer pH 7.4 as 55.56 % to 89.23 ± 0.24 % in 24 hr with reverse electrodialysis system attached and 43.76 % to 81.23 ± 0.14 % in 24 hr without reverse electrodialysis system. The children of different age groups, different body weight with no premedication of anesthetic of analgesic were selected as subjects with written informed consent and divided into two groups depending upon RED system to be attached or not. The patches with and without RED system were attached to forearm of subjects and trial is run. The results obtained showed that patch when attached with reverse electrodialysis system showed greater potential for thermal threshold, lowering of cool sensation and depth of pain. Keywords: Child Anesthesia, Iontophoresis, Reverse Electrodialysis ,Ropivacaine, Transdermal Patch.  

scholarly journals Colon Targeted Protein Nanoparticles Loaded Suppositories : Effective against Intestinal Parasites

2020 ◽  
Vol 11 (3) ◽  
pp. 490-496
Author(s):  
Swati Chauhan ◽  
Neha Jain ◽  
Shilani Sharma ◽  
Shagun Mehra ◽  
Upendra Nagaich
Keyword(s):  
Intestinal Parasites ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic ◽  
Content Uniformity ◽  
Weight Variation ◽  
Protein Nanoparticles ◽  
Release Data ◽  
Average Size

Purpose: The aim of the present investigation was to formulate protein nanoparticles loaded suppositories for colon targeting of metronidazole (MZ), to achieve sustain release effect. Methods: Protein nanoparticles were formulated via desolvation technique by utilizing 2 3 factorial design which results into eight formulations. The synthesized protein nanoparticles were characterized for different physicochemical and in vitro parameters viz. particle size, surface morphology, entrapment efficiency and zeta potential, drug- excipients compatibility studies. Results: The formulated protein nanoparticles were found to be spherical in shape and have an average size in the range of 300.7 nm to 504.8 nm. Based on the results obtained, F7 was found to be the optimized formulation that was loaded into the suppository base. Furthermore, suppositories were also characterized for several parameters like content uniformity, weight variation and liquefaction time. Conclusion: Resultant, suppositories were free from pits, fissures and cracks. The in-vitro release data of metronidazole protein nanoparticles (MZ-PNPs) loaded suppositories were compared with the suppositories loaded with active ingredient only i.e. metronidazole. Screening against Pheretima posthuma was also conducted. The results of in vitro drug release testing proved that protein nanoparticle loaded suppositories is a better approach, compared to pure metronidazole loaded suppositories. Release kinetic study concluded that the formulation follows higuchi’s equation i.e. having a biphasic release pattern. The efficiency of the formulated dosage form was evaluated using Indian earthworms, Pheretima posthuma (P. posthuma).

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