scholarly journals Preparation and Characterization of Chitosan–Alginate Polyelectrolyte Complexes Loaded with Antibacterial Thyme Oil Nanoemulsions

2019 ◽  
Vol 9 (18) ◽  
pp. 3933 ◽  
Author(s):  
Hamid Hamedi ◽  
Sara Moradi ◽  
Alan E. Tonelli ◽  
Samuel M. Hudson
Keyword(s):  
Drug Release ◽  
Uv Spectroscopy ◽  
Drug Carrier ◽  
Antibacterial Properties ◽  
Wound Dressings ◽  
Release Mechanism ◽  
Vapor Permeability ◽  
In Vitro Test ◽  
Thyme Oil

Biomedical industries are attempting to utilize natural materials, as they are bio-compatible, non-toxic, and show bioactive properties, like antimicrobial activity. In this study, natural polyelectrolyte complexed chitosan/alginate films (PECs) were prepared via a casting/solvent evaporation technique, and their characteristics and drug release properties were investigated. PEC films made with two different overall polymer contents, 0.4 and 1 w/v%, were loaded with thyme oil nanoemulsion as drug carrier. The structure of the films was studied by FTIR and optical and scanning electron microscopy. Prepared PEC films had good mechanical and water vapor permeability properties. Release of the thyme oil from the pH-sensitive PEC films (TM-PEC) was detected and followed by UV spectroscopy. The results indicated that the drug release rate of TM-PEC films was the fastest when the chitosan content was 1 %w/v, and various mathematical models were analyzed for investigating the drug release mechanism. Antibacterial tests were performed by counting the number of surviving gram-negative and gram-positive bacteria. The in vitro test indicated the limitation Escherichia coli (E. coli) and Staphylococcus aureus (S.aureus) growth in the presence of TM-PEC films. The MTT test showed more cell viability of the TM-PEC film in comparison with that of the PEC film without TM. Based on the measured physical and antibacterial properties, the chitosan–alginate PEC films loaded with antibacterial essential oils can be considered for biomedical applications, such as wound dressings or controlled release systems.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

scholarly journals Polymer/Iron-Based Layered Double Hydroxides as Multifunctional Wound Dressings

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1130
Author(s):  
Mariana Pires Figueiredo ◽  
Ana Borrego-Sánchez ◽  
Fátima García-Villén ◽  
Dalila Miele ◽  
Silvia Rossi ◽  
...  
Keyword(s):  
Drug Release ◽  
High Performance ◽  
Mechanical Performance ◽  
Release Kinetics ◽  
Wound Dressings ◽  
In Vitro Drug Release ◽  
Improved Performance ◽  
Double Hydroxide ◽  
Double Hydroxides

This work presents the development of multifunctional therapeutic membranes based on a high-performance block copolymer scaffold formed by polyether (PE) and polyamide (PA) units (known as PEBA) and layered double hydroxide (LDH) biomaterials, with the aim to study their uses as wound dressings. Two LDH layer compositions were employed containing Mg2+ or Zn2+, Fe3+ and Al3+ cations, intercalated with chloride anions, abbreviated as Mg-Cl or Zn-Cl, or intercalated with naproxenate (NAP) anions, abbreviated as Mg-NAP or Zn-NAP. Membranes were structurally and physically characterized, and the in vitro drug release kinetics and cytotoxicity assessed. PEBA-loading NaNAP salt particles were also prepared for comparison. Intercalated NAP anions improved LDH–polymer interaction, resulting in membranes with greater mechanical performance compared to the polymer only or to the membranes containing the Cl-LDHs. Drug release (in saline solution) was sustained for at least 8 h for all samples and release kinetics could be modulated: a slower, an intermediate and a faster NAP release were observed from membranes containing Zn-NAP, NaNAP and Mg-NAP particles, respectively. In general, cell viability was higher in the presence of Mg-LDH and the membranes presented improved performance in comparison with the powdered samples. PEBA containing Mg-NAP sample stood out among all membranes in all the evaluated aspects, thus being considered a great candidate for application as multifunctional therapeutic dressings.

scholarly journals In vitro dissolution testing models of ocular implants for posterior segment drug delivery

2021 ◽  
Author(s):  
Muhammad Faris Adrianto ◽  
Febri Annuryanti ◽  
Clive G. Wilson ◽  
Ravi Sheshala ◽  
Raghu Raj Singh Thakur
Keyword(s):  
Drug Release ◽  
Posterior Segment ◽  
In Vitro Dissolution ◽  
Prolonged Treatment ◽  
Term Therapy ◽  
In Vitro Test ◽  
Dissolution Testing ◽  
Vitro Test ◽  
Ocular Implants

AbstractThe delivery of drugs to the posterior segment of the eye remains a tremendously difficult task. Prolonged treatment in conventional intravitreal therapy requires injections that are administered frequently due to the rapid clearance of the drug molecules. As an alternative, intraocular implants can offer drug release for long-term therapy. However, one of the several challenges in developing intraocular implants is selecting an appropriate in vitro dissolution testing model. In order to determine the efficacy of ocular implants in drug release, multiple in vitro test models were emerging. While these in vitro models may be used to analyse drug release profiles, the findings may not predict in vivo retinal drug exposure as this is influenced by metabolic and physiological factors. This review considers various types of in vitro test methods used to test drug release of ocular implants. Importantly, it discusses the challenges and factors that must be considered in the development and testing of the implants in an in vitro setup. Graphical abstract

Development and Evaluation of Trans Buccal Patches based on Natural and Synthetic Polymers Loaded with Rivastigmine using Solvent Casting Technique

2021 ◽  
pp. 5133-5140
Author(s):  
Prasanta Kumar Mohapatra ◽  
Boddu Pavan Kumar ◽  
Pankaj Singh Patel ◽  
Harish Chandra Verma ◽  
Satyajit Sahoo
Keyword(s):  
Drug Release ◽  
Kinetic Equations ◽  
Moisture Loss ◽  
Release Mechanism ◽  
Solvent Casting ◽  
Casting Technique ◽  
Weight Variation ◽  
Zero Order Release ◽  
Buccal Films

Mucoadhesive buccal films of rivastigmine were prepared by the solvent casting technique using HPMC K15M, sodium alginate, glycerine, and Eudragit RL100. Arranged films assessed for weight variation, thickness, % drug substance, % moisture loss, % moisture take-up, folding endurance, in-vitro medicament release, and Fourier transform Infrared spectroscopy (FTIR). The films showed a controlled release (CR) over 8 h. The preparation observed to be a worthy candidate for the development of buccal patches for therapeutic purposes. Drug-polymer compatibility considers FTIR demonstrated no contradiction between the medicament and the polymers. The optimized formulation found F7 indicated drug release 85% at the end of 8 h. Thinking about the correlation coefficient (R2) values got from the kinetic equations, the drug release from the formulations F1-F8 has discovered zero-order release mechanism. It can be concluded that oral buccal patches of rivastigmine, for treatment of Alzheimer’s and Parkinson’s disease, can be formulated. The study suggests that rivastigmine can be conveniently administered orally in the form of buccal patches, with the lesser occurrence of its side effects and improved bioavailability.

FORMULATION AND CHARACTERIZATION OF MEDICATED CHEWING GUMS OF DEXTROMETHORPHAN HYDROBROMIDE

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (12) ◽  
pp. 29-35
Author(s):  
N.G.N Swamy ◽  
◽  
P Shilpa ◽  
Z. Abbas
Keyword(s):  
Drug Release ◽  
Systemic Absorption ◽  
Chewing Gum ◽  
Release Mechanism ◽  
Physical Parameters ◽  
In Vitro Drug Release ◽  
Chewing Gums ◽  
Dextromethorphan Hydrobromide ◽  
Spray Dried

Chewing gums are mobile drug delivery systems, with a potential for administering drugs either for local action or for systemic absorption via buccal route. Dextromethorphan hydrobromide chewing gum formulations were made employing Pharmagum M as the base with an aim to overcome the firstpass effect, reducing the risk of overdosing, ease of administration and for achieving faster systemic absorption. Dextromethorphan hydrobromide was further transformed into spray dried form and incorporated into Pharmagum M base with the object of solubility enhancement and masking the bitter taste of the drug. The prepared medicated chewing gums were evaluated for various precompression and postcompression parameters. The in vitro drug release profiles were carried out employing Erweka DRT chewing apparatus. It was observed that increasing the chewing gum base concentration resulted in a decreased drug release profile. The drug in the spray dried form revealed improved performance in comparison to the directly contained drug. The drug release data were fitted into various kinetic models. It was observed that the drug release was matrix diffusion controlled and revealed a non-Fickian drug release mechanism. Accelerated stability studies were carried out on select formulations as per ICH guidelines. The formulations were found to be stable in respect to physical parameters and no significant deviations were seen in respect to in vitro drug release characteristics.

Preparation and Characterization of Mucoadhesive Microcapsules of Gliclazide with Natural Gums

1970 ◽  
Vol 4 (1) ◽  
pp. 38-48 ◽  
Author(s):  
Santhosh Kumar Mankala ◽  
Nishanth Kumar Nagamalli ◽  
Ramakrishna Raprla ◽  
Rajyalaxmi Kommula
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Guar Gum ◽  
Release Kinetics ◽  
Insulin Dependent Diabetes Mellitus ◽  
Dependent Diabetes Mellitus ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
Release Formulation

Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr’s index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600μm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.   Key words: Gliclazide; Natural gums; orifice ionic gelation technique; emulsification ionic gelation technique DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011; 4(1): 38-48

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

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