scholarly journals Comparison of Rheological, Drug Release, and Mucoadhesive Characteristics upon Storage between Hydrogels with Unmodified or Beta-Glycerophosphate-Crosslinked Chitosan

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Emilia Szymańska ◽  
Anna Czajkowska-Kośnik ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Physicochemical Characteristics ◽  
Vaginal Mucosa ◽  
Drug Release Profile ◽  
Modified Chitosan ◽  
Long Term Storage ◽  
Crosslinked Chitosan ◽  
Chitosan Hydrogels ◽  
The Impact

The physicochemical characteristics of beta-glycerophosphate-crosslinked chitosan hydrogels were investigated upon long-term storage at ambient, accelerated, and refrigerated conditions and compared to unmodified chitosan formulations. Additionally, the impact of chitosan modification on the ex vivo mucoadhesive performance in contact with porcine vaginal mucosa and on the drug release profile from hydrogels was evaluated. Viscosity and mechanical properties of formulations with unmodified chitosan decreased significantly upon storage regardless of tested conditions as a result of hydrolytic depolymerization. Introduction of ion crosslinker exerted stabilizing effect on physicochemical performance of chitosan hydrogels but only upon storage at refrigerated conditions. Beta-glycerophosphate-modified chitosan formulations preserved organoleptic, rheological behavior, and hydrogel structure up to 3-month storage at 4 ± 2°C. Viscosity variations upon storage influenced markedly mucoadhesive properties and drug release rate from hydrogels.

Emulgels Containing Carbopol 934P and Different Vegetable Oils for Topical Propolis Delivery: Bioadhesion, Drug Release Profile, and Ex Vivo Skin Permeation Studies

2020 ◽  
Vol 21 (6) ◽  
Author(s):  
Rafaela Said dos Santos ◽  
Camila Félix Vecchi ◽  
Hélen Cássia Rosseto ◽  
Jéssica Bassi da Silva ◽  
Maria Eduarda Lima Dano ◽  
...  
Keyword(s):  
Drug Release ◽  
Vegetable Oils ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Release Profile ◽  
Drug Release Profile ◽  
Permeation Studies ◽  
Carbopol 934P

scholarly journals Thermoreversible Gel-Loaded Amphotericin B for the Treatment of Dermal and Vaginal Candidiasis

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 312 ◽  
Author(s):  
Lilian Sosa ◽  
Ana Cristina Calpena ◽  
Marcelle Silva-Abreu ◽  
Lupe Carolina Espinoza ◽  
María Rincón ◽  
...  
Keyword(s):  
Drug Release ◽  
Amphotericin B ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Vaginal Candidiasis ◽  
Vaginal Mucosa ◽  
High Porosity ◽  
Candida Spp ◽  
Thermoreversible Gel ◽  
Antifungal Efficacy

The present study was designed to develop a thermoreversible gel of Pluronic (P407) loaded amphotericin B (AmB-gel) for the dermal and vaginal treatment of candidiasis. P407 was used as a copolymer to exploit potential advantages related to increasing drug concentration in the tissue layer in order to provide a local effect. Parameters including internal structure, swelling, porosity, and short-term stability were determined. In addition, drug release profile and ex vivo skin and vaginal permeation studies were carried out. Antifungal efficacy was evaluated against strains of Candida spp. and atomic force microscopy (AFM) supported the results. The tolerance of AmB-gel was studied by evaluating biomechanical properties of skin and determining the irritation level in scarified rabbit skin supported by histological analysis. Results confirmed the development of a thermoreversible AmB-gel with high porosity exhibiting Newtonian behavior at 4 °C and pseudoplasticity at 32 °C as well as optimal stability for at least 90 days. The Amb-gel provided a sustained drug release following a Boltzmann sigmoidal model. Non permeation was observed in skin and vaginal mucosa, showing a high retained amount of AmB of 960.0 and 737.3 µg/g/cm2, respectively. In vitro antifungal efficacy showed that AmB-gel was more effective than Free-AmB in inhibiting strains of Candida spp. and these results were corroborated by AFM. Finally, tolerance studies showed that its application did not induce skin irritation nor alter its biophysical properties. Together, these results confirmed that AmB-gel could be proposed as a promising candidate for the clinical status in the treatment of skin and vaginal candidiasis.

scholarly journals FORMULATION AND EVALUATION OF METRONIDAZOLE MICROSPHERES-LOADED BIOADHESIVE VAGINAL GEL

2017 ◽  
Vol 10 (3) ◽  
pp. 418
Author(s):  
Banasmita Kalita ◽  
Kritika Saikia ◽  
Bhupen Kalita
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Spherical Particles ◽  
Vaginal Fluid ◽  
Vaginal Mucosa ◽  
Scanning Calorimetry ◽  
Vaginal Gel ◽  
Study Results

ABSTRACTObjectives: The objective of the present work is to develop and characterize metronidazole microsphere-loaded bioadhesive vaginal gel to ensurelonger residence time at the infection site, providing a favorable release profile for the drug.Methods: Microsphere was prepared by solvent evaporation method in various ratios of metronidazole to poly-ε-caprolactone (PCL). Physicochemicalevaluation of microspheres includes determination of solubility in simulated vaginal fluid, partition coefficient (n-octanol/citrate phosphatebuffer pH 4.5), particle size distribution, entrapment efficiency, X-ray diffraction, and surface morphology by scanning electron microscopy (SEM).Drug excipient compatibility was established by Fourier transform infrared and differential scanning calorimetry studies. Bioadhesive gel wasprepared using Carbopol 934P and HPMC K4M in various concentrations, and methyl paraben was used as a preservative. The pH was adjustedwith triethanolamine which resulted in a translucent gel. The optimized metronidazole microsphere formulation was dispersed into the gel base.Microspheres in gel formulations were evaluated for pH, viscosity, spreadability, drug content, and gelling strength. Ex vivo mucoadhesive strength ofthe gel was determined on goat vaginal mucosa. In vitro drug release study was performed using cellophane membrane.Results: The optimized batch of microsphere F4 (drug-polymer ratio 1:4) showed entrapment efficiency of 72.62±3.66%, solubility of 1.5 mg/ml, andpartition coefficient of 0.12. Particle size of all the formulations was observed below 100 μm. Regular and spherical particles were observed in theSEM photomicrographs. The optimized gel formulation G5 (Carbopol and HPMC at 1: 0.25 ratio) showed viscosity of 7538 cps at 100 RPM, gel strengthrecorded as 35 secobds for a 1000.00 mg load, and spreadability of 4.6 g.cm/seconds. G5 showed 82.4% drug release at 10.0 hrs and mucoadhesivestrength of 6.5±1.2 g.Conclusion: The study results suggest that metronidazole-loaded PCL microsphere in mucoadhesive gel would provide a mean for sustainedtreatment of vaginal infections.Keywords: Microsphere, Metronidazole, Bioadhesive vaginal gel.

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 Critical Factors for Metformin Osmotic Controlled Release Pump

2020 ◽  
pp. 1-12
Author(s):  
García-Flores Mirna ◽  
Melgoza-Contreras Luz María ◽  
Hernández-Baltazar Efrén
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Osmotic Pump ◽  
Critical Factors ◽  
Scanning Electronic Microscopy ◽  
Electronic Microscopy ◽  
Drug Release Profile ◽  
Osmotic Pumps ◽  
The Impact

Aim: Studied the critical factors in the design of an osmotic pump with metformin release rate constant at 4%/hr in diabetes mellitus within 24 hr. with the goal to reduce daily medications. Study Design: Experimental design 32 Methodology: In vitro drug release profiles for 24h. The effects of different formulation variables, that is, concentration of hydrophilic polymer, diameter of drug releasing orifice and coating thickness, on the drug release profile were investigated. Also, the impact of pH, osmotic pressure and morphology with stereo microscopy and scanning electronic microscopy of the osmotic pumps were investigated. At last, osmotic pumps surface was analyze with scanning electronic microscopy. Results: Metformin osmotic pump were successfully prepared in this study to overcome the weak point of multiple doses and great concentration fluctuation of metformin. The formulation determined finally have a release orifice of 700 mm and 3.0% of weight gain, achieved the desired effect which can realize the constant drug release rate at the first 24 hr. Conclusion: The developed osmotic systems have a linear release near 4%/hr. and demonstrated that the behavior was independent of the agitation intensity and the pH of the gastrointestinal apparatus.

scholarly journals A COMPARATIVE STUDY OF TERBINAFINE ETHOSOMAL FORMULATIONS: A NOVEL APPROACH

2013 ◽  
Vol 03 (04) ◽  
pp. 023-029
Author(s):  
Narayana Charyulu R. ◽  
Mehta Satveek ◽  
Harish N. M. ◽  
Amit B. Patil
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Comparative Investigation ◽  
Drug Accumulation ◽  
Dose Frequency ◽  
The Impact

AbstractThe present research work aimed at the impact of reduced vesicular size on the characteristics of ethosomes by comparing with the regular vesicular size of ethosomes as topical drug delivery vehicle to achieve optimal localized drug concentration and reduced dose frequency of the Terbinafine hydrochloride (TH), an antifungal drug. Oral use of TH contraindicated resulting from sever side effect, thus topical administration is recommended. Commercially available TH creams, lotions and sprays, have limitation of relatively short residual period at target site. The entrapment of drug in vesicles improves localization, solubility and availability of drug at the site; resulting in reduction of the dose. Ethosomes containing drug were prepared by employing higher concentration of alcohol in the form of hydroalcoholic or hydroglycolic phospholipid. Sonicated and unsonicated ethosomes were investigated for shape, particle size, and entrapment efficiency. Electronic microscope investigation not only revealed, vital evidence for presence of phospholipid vesicles in TH ethosomal systems but also displayed greater uniformity in size and shape of sonicated ethosomes than unsonicated ethosomes. Furthermore, the Comparative investigation was carried out for ex vivo skin permeation, ex vivo drug release and entrapment efficiency studies. Drug release followed zero order release rate kinetics. Drug accumulation study showed more than 19.01 % of drug was deposited into skin by sonicated ethosomal formulation as compared to 2.57 % by unsonicated ethosomal formulation. Sonicated and unsonicated ethosomes were found stable at refrigeration and room temperature conditions during stability studies. Drug accumulation studies in deep skin strata was found to be comparatively greater in sonicated ethosomes, which indicates higher localized drug and that in turn reduces dose frequency.

scholarly journals Evaluation of Influence of Various Polymers on Dissolution and Phase Behavior of Carbamazepine-Succinic Acid Cocrystal in Matrix Tablets

2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Majeed Ullah ◽  
Hanif Ullah ◽  
Ghulam Murtaza ◽  
Qaisar Mahmood ◽  
Izhar Hussain
Keyword(s):  
Drug Release ◽  
Succinic Acid ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Inverse Relation ◽  
Direct Relation ◽  
Drug Release Profile ◽  
X Ray ◽  
Opposite Trend ◽  
The Impact

The aim of current study was to explore the influence of three commonly used polymers, that is, cellulosics and noncellulosics, for example, Methocel K4M, Kollidon VA/64, and Soluplus, on the phase disproportionation and drug release profile of carbamazepine-succinic acid (CBZ-SUC) cocrystal at varying drug to polymer ratios (1 : 1 to 1 : 0.25) in matrix tablets. The polymorphic phase disproportionation during in-depth dissolution studies of CBZ-SUC cocrystals and its crystalline properties were scrutinized by X-ray powder diffractrometry and Raman spectroscopy. The percent drug release from HPMC formulations (CSH) showed inverse relation with the concentration of polymer; that is, drug release increased with decrease in polymer concentration. On contrary, direct relation was observed between percent drug release and polymer concentrations of Kollidon VA 64/Soluplus (CSK, CSS). At similar polymer concentration, drug release from pure carbamazepine was slightly lower with HPMC formulations than that of cocrystal; however, opposite trend in release rate was observed with Kollidon VA/64 and Soluplus. The significant increase in dissolution rate of cocrystal occurred with Kollidon VA/64 and Soluplus at higher polymer concentration. Moreover, no phase change took place in Methocel and Kollidon formulations. No tablet residue was left for Soluplus formulation so the impact of polymer on cocrystal integrity cannot be predicted.

scholarly journals Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

2021 ◽  
Vol 14 (1) ◽  
pp. 68
Author(s):  
Eman A. Mazyed ◽  
Doaa A. Helal ◽  
Mahmoud M. Elkhoudary ◽  
Ahmed G. Abd Elhameed ◽  
Mohamed Yasser
Keyword(s):  
Drug Release ◽  
Pharmacokinetic Study ◽  
Ex Vivo ◽  
Epigallocatechin Gallate ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Ethanol Injection ◽  
23 Factorial Design ◽  
The Impact

The present study aimed to investigate the potential of nanospanlastics for boosting the bioavailability of epigallocatechin gallate (EGCG). EGCG has valuable effects like anti-inflammation, anti-oxidation, and anti-tumorigenesis. Unfortunately, it has a low oral bioavailability due to its limited permeation and poor stability. To overcome these pitfalls, EGCG was fabricated as a nanospanlastic. Nanospanlastics are flexible nanovesicles that are composed of surfactants and edge activators (EAs). EAs improve the deformability of spanlastics by acting as a destabilizing factor of their vesicular membranes. EGCG-loaded spanlastics were prepared by an ethanol injection method, according to 23 factorial design, to explore the impact of different independent variables on entrapment efficiency (EE%), % drug released after 12 h (Q12h), and particle size (PS). In vitro characterization, ex vivo intestinal permeation test, and pharmacokinetic study of the optimized formula were performed. A newly developed RP-HPLC technique was adopted for the estimation of EGCG. The optimized formula (F4) demonstrated more prolonged drug release and a significant improvement in the EE%, permeability, deformability and stability than the corresponding niosomes. The pharmacokinetic study investigated that F4 had a more sustained drug release and a higher bioavailability than the conventional niosomes and free drugs. Nanospanlastics could be a promising approach for improving the bioavailability of EGCG.

Fabrication of cefixime nanoparticles loaded films and their ex vivo antimicrobial effect on periodontitis patient’s saliva

2021 ◽  
Vol 10 ◽  
Author(s):  
Rakeshkumar Parmar ◽  
Mohammad Salman M ◽  
Payal Chauhan
Keyword(s):  
Molecular Weight ◽  
Drug Release ◽  
Ex Vivo ◽  
Chitosan Film ◽  
Inhibition Zone ◽  
Release Profile ◽  
Low Molecular Weight ◽  
Drug Release Profile ◽  
Low Molecular Weight Chitosan

Aim: This study was designed to prepare and evaluate cefixime-loaded nanoparticles containing low molecular weight chitosan films for the enhanced topical treatment of periodontitis. Methods: To fabricate the enhanced antimicrobial films, a nanoprecipitation method for cefixime nanoparticles followed by a solvent evaporation method for these nanoparticles loaded films were adopted in this study. Nine batches of nanoparticles (NPs) with different concentrations of ethyl cellulose and polyvinyl alcohol were prepared and evaluated. Furthermore, nine batches of optimized NPs loaded films with different concentrations of low molecular weight chitosan and glycerol were fabricated and evaluated. Optimized NPs loaded films were assessed for their antimicrobial activity against the periodontitis patient’s saliva samples. Results: The FT-IR spectroscopy and XRD study revealed that there was no interaction between the drug and all other excipients and the drug remained amorphous form in chitosan film. The SEM study revealed that the prepared NPs were spherical in shape and uniformly distributed in chitosan film. In vitro drug release study revealed the NPs have a sustained release profile up to 8 days and NPs loaded films have up to 11 days. The conventional marketed mouth wash shows a low inhibition zone of 5.70 ± 0.043 mm, whereas NPs loaded film shows a higher inhibition zone of 6.72 ± 0.063 mm against periodontal microorganisms present in the patient’s saliva. The stability study revealed that the optimized NPs loaded film shows no dramatic change in drug release profile and folding endurance after six months. Conclusion: This present study highlights the possible usage of cefixime NPs loaded films in enhanced periodontal treatment.

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