scholarly journals Chlorhexidine Mucoadhesive Buccal Tablets: The Impact of Formulation Design on Drug Delivery and Release Kinetics Using Conventional and Novel Dissolution Methods

2021 ◽  
Vol 14 (6) ◽  
pp. 493
Author(s):  
Enas Al-Ani ◽  
David Hill ◽  
Khalid Doudin
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Poloxamer 407 ◽  
Oropharyngeal Candidiasis ◽  
Scanning Calorimetry ◽  
Buccal Tablets ◽  
The Impact

Oropharyngeal candidiasis (OPC) is a mucosal infection caused by Candida spp., and it is common among the immunocompromised. This condition is mainly treated using oral antifungals. Chlorhexidine (CHD) is a fungicidal and is available as a mouth wash and oral gel. It is used as an adjuvant in the treatment of OPC due to the low residence time of the current formulations. In this study, its activity was tested against C. albicans biofilm and biocompatibility with the HEK293 human cell line. Then, it was formulated as mucoadhesive hydrogel buccal tablets to extend its activity. Different ratios of hydroxypropyl methylcellulose (HPMC), poloxamer 407 (P407), and three different types of polyols were used to prepare the tablets, which were then investigated for their physicochemical properties, ex vivo mucoadhesion, drug release profiles, and the kinetics of drug release. The release was performed using Apparatus I and a controlled flow rate (CFR) method. The results show that CHD is biocompatible and effective against Candida biofilm at a concentration of 20 µg/mL. No drug excipient interaction was observed through differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). The increase in P407 and polyol ratios showed a decrease in the swelling index and an increase in CHD in vitro release. The release of CHD from the selected formulations was 86–92%. The results suggest that chlorhexidine tablets are a possible candidate for the treatment of oropharyngeal candidiasis.

scholarly journals Evaluation of Transdermal Formulations of Metoclopramide Prepared Using Arachis Oil and Liquid Paraffin as Permeation Enhancers

2020 ◽  
Author(s):  
Sylvester O. Eraga ◽  
Matthew I. Arhewoh ◽  
Ogochukwu A. Meko
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Liquid Paraffin ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Tween 80 ◽  
Patient Acceptance ◽  
Scanning Calorimetry

Background: The study aimed to evaluate the effect of arachis oil and liquid paraffin on metoclopramide release from transdermal films. Objectives: Batches of metoclopramide films were prepared with hydroxypropyl methyl cellulose (HPMC), arachis oil or liquid paraffin and Tween 80 as plasticizer. The films were evaluated for their physiochemical properties, in vitro and ex vivo drug release and drug release kinetics. Drug-excipient interactions were investigated using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared (FTIR) spectroscopy. Methods: The transdermal films had a weight range of 0.22-0.24 g, folding endurance of 300-306, percentage moisture content and uptake of 2%-10% and 19%-110%, respectively and drug content of 98%-104%. There was similar condition in vitro release profile for the films but their ex vivo profiles exhibited variable drug release with the P3 (30% arachis oil) giving the highest drug (almost 100%) release.  Results: The release kinetics of metoclopramide followed the first order and Korsemeyer-Peppas models more closely as seen in their correlation coefficients (R2) of 0.9832 and 0.9560, respectively. Drug-excipient compatibility studies showed no interactions between excipients and metoclopramide. Conclusion: The formulated transdermal films showed controlled drug release over a period of 12 h. Arachis oil and liquid paraffin showed similar permeation enhancing ability. These enhanced permeation properties of the films could be helpful in the development of alternative route for metoclopramide administration in the management of emesis with improved patient acceptance.

scholarly journals Spray-Formed Layered Polymer Microneedles for Controlled Biphasic Drug Delivery

Polymers ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 369 ◽  
Author(s):  
Seok Park ◽  
Min Kim ◽  
Seung-Ki Baek ◽  
Jung-Hwan Park ◽  
Seong-O Choi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Diffusion Barrier ◽  
Structural Changes ◽  
Tertiary Structure ◽  
Ex Vivo ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Drug Delivery System ◽  
Initial Burst

In this study we present polymeric microneedles composed of multiple layers to control drug release kinetics. Layered microneedles were fabricated by spraying poly(lactic-co-glycolic acid) (PLGA) and polyvinylpyrrolidone (PVP) in sequence, and were characterized by mechanical testing and ex vivo skin insertion tests. The compression test demonstrated that no noticeable layer separation occurred, indicating good adhesion between PLGA and PVP layers. Histological examination confirmed that the microneedles were successfully inserted into the skin and indicated biphasic release of dyes incorporated within microneedle matrices. Structural changes of a model protein drug, bovine serum albumin (BSA), in PLGA and PVP matrices were examined by circular dichroism (CD) and fluorescence spectroscopy. The results showed that the tertiary structure of BSA was well maintained in both PLGA and PVP layers while the secondary structures were slightly changed during microneedle fabrication. In vitro release studies showed that over 60% of BSA in the PLGA layer was released within 1 h, followed by continuous slow release over the course of the experiments (7 days), while BSA in the PVP layer was completely released within 0.5 h. The initial burst of BSA from PLGA was further controlled by depositing a blank PLGA layer prior to forming the PLGA layer containing BSA. The blank PLGA layer acted as a diffusion barrier, resulting in a reduced initial burst. The formation of the PLGA diffusion barrier was visualized using confocal microscopy. Our results suggest that the spray-formed multilayer microneedles could be an attractive transdermal drug delivery system that is capable of modulating a drug release profile.

Formulation and Ex-vivo Evaluation of Glipizide Buccal Tablets

2014 ◽  
Vol 7 (2) ◽  
pp. 2487-2493
Author(s):  
Sudarshan Singh ◽  
Sandip G Maru ◽  
Sunil Bothara B
Keyword(s):  
Guar Gum ◽  
Chemical Interaction ◽  
Ex Vivo ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Aloe Vera ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Buccal Tablets

Bioadhesive materials are agents which adhere to the mucous membrane due to specific properties and release the drug at the site of action in controlled manner. Since the biodegradability of the synthetic polymer is at some instance hesitant. In this exploration, a bioadhesive polymer has been developed which was isolated from leaves of Aloe vera (L.) Burm. f. The mucilage isolated from A. vera were used as a bioadhesive polymer in tablet formulation and evaluated for the parameters such as swelling, pH, and bioadhesive property like bioadhesive strength, record of adherence and ex-vivo residence time. The buccal bioadhesive tablet was prepared using glipizide as model drug. The prepared tablet was evaluated against existing bioadhesive polymer such as guar gum and hydroxyl propyl cellulose. Swelling index and surface pH was found to be 13.12-18.06% and 6.5-6.9 respectively. The drug permeation through goat buccal mucosa was found to be 60.21 ± 0.06 % in the end of 7 h with a Jss of 0.24 mg h-1 cm-2. The stability studies were performed on optimized formulation as per ICH guideline, result showed that there was no significant change in physical characteristic, adhesive strength and in vitro release. It was observed that as the concentration of mucilage increases swelling index also increases. Results of pH showed that mucilage is slightly near to neutral in nature. Formulations were evaluated for preformulation parameters, in vitro drug release profile and release kinetics. The formulations were found to have good preformulation characteristics. FTIR spectroscopy showed no significant chemical interaction within drug and excipients. The release mechanism of glipizide from buccal tablets indicated anomalous (non-fickian) transport mechanism and followed zero order kinetics. It was concluded that the mucilage of A. vera can be used as a pharmaceutical excipient in buccal bioadhesive drug delivery systems.

Fast Dissolving Sublingual Strips: A Novel Approach for the Delivery of Isosorbide Dinitrate

2019 ◽  
Vol 25 (4) ◽  
pp. 311-318
Author(s):  
Marzieh Fathei ◽  
Mitra Alami-milani ◽  
Sara Salatin ◽  
Sharahm Sattari ◽  
Hassan Montazam ◽  
...  
Keyword(s):  
Drug Release ◽  
Isosorbide Dinitrate ◽  
Moisture Absorption ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Drug Bioavailability ◽  
Scanning Calorimetry ◽  
Surface Ph ◽  
Drug Content

Background: Isosorbide dinitrate (ISDN) is used for treating the angina attacks. In addition, oral ISDN is available in immediate and sustained release formulations and the bioavailability of ISDN is about 20-25% when taken orally. Further, the ISDN films are developed for sublingual drug delivery by improving drug bioavailability. The present study aimed to design and evaluate the physicochemical properties of the film formulation for sublingual delivery of ISDN. Methods: In the present study, sublingual films were prepared by the solvent casting technique using the hydroxypropyl methylcellulose (HPMC) polymers (i.e., 100, 150 and 200 mg) with a different drug to polymer ratios (i.e., 1:5, 1:7.5 and 1:10). Then, ISDN was evaluated for the film appearance, drug content, surface pH, mucoadhesion force, differential scanning calorimetry (DSC), in vitro drug release, and ex vivo permeability. Results: Based on the results, F3 formulation (1:10 ISDN to HPMC ratio) showed acceptable thickness (0.93 mm), weight (11.14 mg), surface pH (7.82), moisture absorption capacity (6.08%), elasticity (>200), mucoadhesion force (18.05 N/cm2), and drug content (6.22%). Furthermore, the results demonstrated that HPMC polymer improved the characteristics of the films, modified the bioadhesiveness, and finally, enhanced elasticity. However, DSC thermogram failed to show any crystalline drug substance in the films except for F1 (immediate release) and the endothermic peak of ISDN was absent in F2 and F3 films. Therefore, the drug which was entrapped into the film was in an amorphous or disturbed-crystalline phase of the molecular dispersion or dissolved in the melted polymer in the polymeric matrix. Moreover, the drug release from the films was faster compared to the tablet® (P<0.05). Conclusion: In general, the formulation of F1 was observed to be an appropriate candidate for developing the sublingual film for the remedial use.

DEVELOPMENT OF FLOATING GASTRORETENTIVE DRUG DELIVERY SYSTEM BASED ON A NOVEL EXCIPIENT FOR METFORMIN HYDROCHLORIDE USING MIXTURE DESIGN

2020 ◽  
pp. 62-71
Author(s):  
R. PAWAR ◽  
S. JAGDALE ◽  
D. RANDIVE
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Mixture Design ◽  
Release Profile ◽  
Metformin Hydrochloride ◽  
Matrix Tablet ◽  
Vitro Release

Objective: The present study aimed to develop a new SR metformin hydrochloride (MH) gastroretentive formulation with novel excipient (NE), which has better floatation and can be prepared with more simple pharmaceutical techniques for the treatment of diabetes Mellitus. Methods: A gastro-retentive floating matrix tablet (GFT) formulation of MH was prepared using various concentrations of PEO (Polyox WSR-303) and hydroxypropyl methylcellulose K100M (HPMC K100 M) and Floating agent (novel excipient) to achieve desirable TFT, FLT and drug release. The wet granulation method was selected using isopropyl alcohol as a binder for the preparation of tablets. D-optimal non-simplex mixture design was used for the selection of suitable polymer concentrations and floating agents. Release kinetics was used to determine the mechanism of drug release. Results: It was observed that GFT with optimum quantities of PEO, HPMC K100M, and the floating agent showed 100 % of drug release in 24h with FT up to 24h and minimum FLT of less than 2 min. Formulation with an in vitro release profile slower to the marketed sample was prepared. Conclusion: A sustained-release (GFT) of MH tablets using PEO-, HPMC K100M, and an effervescent system was successfully prepared. AGFT formulation with an in vitro release profile slower to the marketed sample that releases MH for 24h may suitable for once-daily dosing can be prepared.

Silver sulfadiazine loaded breathable hydrogel sponge for wound healing

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Anamika Pandey ◽  
Munira Momin ◽  
Anita Chando
Keyword(s):  
Wound Healing ◽  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Antimicrobial Property ◽  
Morphological Characteristics ◽  
Silver Sulfadiazine ◽  
Scanning Calorimetry ◽  
Casting Technique

AbstractObjectivesPatients with serious injury need special care and treatment to control the infection, as wound sepsis is one of the major causes of death. Silver sulfadiazine (SSD) is widely used as an antimicrobial agent which promotes healing and re-epithelialization. However, due to certain drawbacks such as inflammation and cytotoxicity, the need for novel drug delivery modality emerges. The objective of this study was to develop natural polymeric (chitosan and gelatin) hydrogel sponges containing SSD and evaluate its efficacy in wound healing using animal models.MethodsSSD containing hydrogel sponges were prepared by solvent casting technique. Scanning electron microscopy (SEM) and Differential scanning calorimetry (DSC) were used to evaluate morphological characteristics of the hydrogel sponges. Anti-thrombogenic property, drug release studies, drug release kinetics, antimicrobial property, and wound healing effect were also studied in detail.ResultsThe optimized batch of hydrogel sponges (CG4) consists of 1% SSD wt., 10% wt. Gelatin, 1% wt. Chitosan and honey 7.5% wt. as plasticizer. At the 12th hour, in vitro and ex vivo drug release was found to be 76.994±0.67% and 24.22±0.57% respectively. CG4 batch had enhanced in vitro antimicrobial activity as compared to conventional marketed cream. The developed SSD hydrogel sponges showed a faster rate of wound healing as compared to a marketed cream. Animals treated with CG4 formulation showed complete angiogenesis and re-epithelialization by 8th day, whereas 12 days were required for complete wound healing with marketed cream.ConclusionsThe prepared hydrogel sponges can serve as a potential alternative for wound healing dressing as compared to the marketed product.

scholarly journals DESIGN OF CONTROLLED RELEASE MUCOADHESIVE BUCCAL TABLETS OF IVABRADINE HCL USING SINTERING TECHNIQUE

2021 ◽  
pp. 192-203
Author(s):  
CHANDAN MOHANTY ◽  
K. V. SUBRAHMANYAM
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Ex Vivo ◽  
Diffusion Mechanism ◽  
Hydroxypropyl Methylcellulose ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Stability Studies ◽  
Buccal Tablets

Objective: The objective of the present work was to study the use of the sintering technique, a relatively new concept in pharmaceutical sciences, in the development of mucoadhesive buccal tablets for ivabradine Hydrochloride. Methods: The method consisted of blending drug, hydroxypropyl methylcellulose (HPMC K100M), carnauba wax, and other excipients followed by direct compression into tablets. The compressed fluffy matrices were sintered at two different constant temperatures like 50 °C and 60 °C for two different periods like 1.5 h and 3 h in a hot air oven. The effect of sintering on tensile strength, dissolution profile, and other parameters were studied. The drug-polymer-excipient compatibility was evaluated by Fourier transform Infrared (FTIR) and differential scanning calorimetric (DSC) studies. Results: The sintering condition markedly affected the drug release properties, hardness, and friability of the tablets. Based on the f2 similarity factor value, Ex-vivo mucoadhesive strength, Ex-vivo residence time, and in vitro dissolution studies, formulation F3SD was selected as an optimized formulation. Drug release followed a non-Fickian diffusion mechanism with the Higuchi model release kinetics. Stability studies of mucoadhesive buccal tablets in normal human saliva indicated the stability of the drug and buccal tablet in the oral cavity. Stability studies as per ICH guidelines revealed that optimized formulation was stable on storage conditions. Conclusion: The sintering technique provides a significant and convenient method for the development of a controlled release dosage form that can be used in the design of mucoadhesive buccal tablets of Ivabradine HCL.

Development and Characterization of Water-in-Oil Microemulsion for Transdermal Delivery of Eperisone Hydrochloride

2020 ◽  
Vol 7 (1) ◽  
pp. 45-64
Author(s):  
Monika D. Kumbhar ◽  
Manisha S. Karpe ◽  
Vilasrao J. Kadam
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Droplet Size ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Tween 80 ◽  
Physical Parameters ◽  
Scanning Calorimetry ◽  
Spontaneous Emulsification

Background: Eperisone hydrochloride possesses short biological half-life due to first pass metabolism resulting in low bioavailability and short duration of response with toxic effects, ultimately limits its utilization for treatment of muscle spasm. Objective: In view of this background, current study was designed for the development of Eperisone hydrochloride-loaded microemulsion and Eperisone hydrochloride-loaded microemulsion based cream for topical delivery and compared it with conventional cream. Methods: Firstly, water-in-oil microemulsion was prepared by spontaneous emulsification method. The concentration of components was found out from existence of microemulsion region by constructing pseudoternary phase diagram. The oil was selected on the basis of drug solubility effect on the drug release, whereas surfactant and cosurfactant were screened on the basis of their efficiency to form microemulsion region. The influence of components on microemulsion formation, drug release capacity, permeation was studied by differential scanning calorimetry, X-ray diffraction, in-vitro release and ex-vivo drug permeation studies respectively. By using microemulsion, the cream was prepared for proving optimum structure for topical application. Microemulsion was evaluated for droplet size, zeta potential, pH, viscosity and conductivity. Besides the cream was characterized for pH, rheology and stability. Permeation of EPE from microemulsion across the rat skin was evaluated and compared with conventional cream. Results: The microemulsion consisting Isopropyl Myristrate/Water/Span 80:Tween 80 (50/8/42% by weight) possessed droplet size of 95.77nm, zeta potential of −5.23 mV with 7.25 pH and conductivity near to zero (<0.05mScm-1). Physical parameters of the cream were satisfactory, also 2.33-fold higher permeation and 1.57-fold higher release observed as compared to conventional cream. Conclusion: It can be concluded that Eperisone hydrochloride-loaded microemulsion and its cream is being effectively used for muscle spasticity by topical route.

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.

Novel Herbal Topical Patch Containing Curcumin and Arnica montana for the Treatment of Osteoarthritis

2020 ◽  
Vol 16 (1) ◽  
pp. 43-60 ◽  
Author(s):  
Priyanka Kriplani ◽  
Kumar Guarve ◽  
Uttam Singh Baghel
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Analgesic Activity ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Methyl Cellulose ◽  
World Population ◽  
Jojoba Oil ◽  
Arnica Montana ◽  
Transdermal Patches

Background: Osteoarthritis (OA) ranks fifth among all forms of disability affecting 10% of the world population. Current treatments available are associated with multiple side effects and do not slow down the progression of the disease. Moreover, no such effective treatment is available to date in various systems of medicine to treat osteoarthritis. Curcumin and Arnica have shown evident clinical advances in the treatment of osteoarthritis. Objective: The aim of the present study was to design, optimize and characterize novel herbal transdermal patches of curcumin and Arnica montana using factorial design. Methods: A multiple factorial design was employed to investigate the effect of hydroxypropyl methyl cellulose, ethyl cellulose and jojoba oil on elongation and drug release. Transdermal patches were evaluated by FTIR, DSC, FESEM, ex vivo drug permeation, anti osteoarthritic activity and analgesic activity. Results: Independent variables exhibited a significant effect on the physicochemical properties of the prepared formulations. The higher values of drug release and elongation were observed with the higher concentration of hydroxypropyl methylcellulose and jojoba oil. Anti osteoarthritic activity was assessed by complete Freund's adjuvant arthritis model; using rats and analgesic activity by Eddy's hot plate method, using mice. Combination patch exhibited good anti osteoarthritic and analgesic activity as compare to individual drug patches. Conclusion: The design results revealed that the combination patch exhibited good physicochemical, anti osteoarthritic and analgesic activity for the treatment of osteoarthritis in animals. More plants and their combinations should be explored to get reliable, safe and effective formulations that can compete with synthetic drugs.

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