scholarly journals Mucoadhesive Gelatin Buccal Films with Propranolol Hydrochloride: Evaluation of Mechanical, Mucoadhesive, and Biopharmaceutical Properties

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 273
Author(s):  
Marija Jovanović ◽  
Nataša Tomić ◽  
Sandra Cvijić ◽  
Dušica Stojanović ◽  
Svetlana Ibrić ◽  
...  
Keyword(s):  
In Silico ◽  
Drug Transport ◽  
In Vitro Release ◽  
Work Of Adhesion ◽  
Therapeutic Drug ◽  
Propranolol Hydrochloride ◽  
Scanning Calorimetry ◽  
In Silico Simulation ◽  
Buccal Films

This study processes and characterizes propranolol hydrochloride/gelatin mucoadhesive buccal films. Two types of gelatin are used: Gelatin from porcine skin, type A (GA), and gelatin from bovine skin (GB). The influence of gelatin type on mechanical, mucoadhesive, and biopharmaceutical characteristics of buccal films is evaluated. Fourier-Transfer infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) analysis show that GA with propranolol hydrochloride (PRH) in the film (GAP) formed a physical mixture, whereas GB with PRH (GBP) form a compound-complex. Results of mechanical testing (tensile test, hardness) revealed that GAP films exhibit higher elastic modulus, tensile strength, and hardness. A mucoahesion test shows that GBP has higher adhesion strength, while GAP shows higher work of adhesion. Both in vitro release study and in silico simulation indicated that processed films can provide effective drug transport through the buccal mucosa. In silico simulation shows improved bioavailability from buccal films, in comparison to the immediate-release tablets—indicating that the therapeutic drug dose can be markedly reduced.

scholarly journals Effect of Doxycycline Microencapsulation on Buccal Films: Stability, Mucoadhesion and In Vitro Drug Release

Gels ◽  
2021 ◽  
Vol 7 (2) ◽  
pp. 51
Author(s):  
Venu Gopal Reddy Patlolla ◽  
Nikolina Popovic ◽  
William Peter Holbrook ◽  
Thordis Kristmundsdottir ◽  
Sveinbjörn Gizurarson
Keyword(s):  
Tensile Strength ◽  
Room Temperature ◽  
In Vitro Release ◽  
Sodium Thiosulfate ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Metalloproteinase Inhibitors ◽  
The Stability ◽  
Buccal Films

The aim of this work was to stabilize doxycycline in mucoadhesive buccal films at room temperature (25 °C). Since doxycycline is susceptible to degradation such as oxidation and epimerization, tablets are currently the only formulation that can keep the drug fully stable at room temperature, while liquid formulations are limited to refrigerated conditions (4 °C). In this study, the aim was to make formulations containing subclinical (antibiotic) doxycycline concentration that can act as matrix metalloproteinase inhibitors (MMPI) and can be stored at temperatures such as 25 °C. Here, doxycycline was complexed with excipients using three techniques and entrapped into microparticles that were stored at 4 °C, 25 °C and 40 °C. Effect of addition of precomplexed doxycycline microparticles on films: stability mucoadhesion capacity, tensile strength, swelling index and in vitro release was studied. The complexation efficiency between drug-excipients, microparticles and films was studied using Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Two of the films were found to be stable at 4 °C but the film containing microparticle composed of precomplexed doxycycline with β-cyclodextrin, MgCl2, sodium thiosulfate, HPMC and Eudragit® RS 12.5 was found to be stable at 25 °C until 26 weeks. The addition of microparticles to the films was found to reduce the mucoadhesive capacity, peak detachment force, tensile strength and elasticity, but improved the stability at room temperature.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals Phycobilins as Potent Food Bioactive Broad-Spectrum Inhibitors Against Proteases of SARS-CoV-2 and Other Coronaviruses: A Preliminary Study

2021 ◽  
Vol 12 ◽  
Author(s):  
Brahmaiah Pendyala ◽  
Ankit Patras ◽  
Chandravanu Dash
Keyword(s):  
Binding Affinity ◽  
Broad Spectrum ◽  
In Silico ◽  
Research Area ◽  
Therapeutic Drug ◽  
Inhibitor Activity ◽  
Current Vaccine ◽  
Mutant Strains ◽  
The Impact

In the 21st century, we have witnessed three coronavirus outbreaks: SARS in 2003, MERS in 2012, and the ongoing pandemic coronavirus disease 2019 (COVID-19). The search for efficient vaccines and development and repurposing of therapeutic drugs are the major approaches in the COVID-19 pandemic research area. There are concerns about the evolution of mutant strains (e.g., VUI – 202012/01, a mutant coronavirus in the United Kingdom), which can potentially reduce the impact of the current vaccine and therapeutic drug development trials. One promising approach to counter the mutant strains is the “development of effective broad-spectrum antiviral drugs” against coronaviruses. This study scientifically investigates potent food bioactive broad-spectrum antiviral compounds by targeting main protease (Mpro) and papain-like protease (PLpro) proteases of coronaviruses (CoVs) using in silico and in vitro approaches. The results reveal that phycocyanobilin (PCB) shows potential inhibitor activity against both proteases. PCB had the best binding affinity to Mpro and PLpro with IC50 values of 71 and 62 μm, respectively. Also, in silico studies with Mpro and PLpro enzymes of other human and animal CoVs indicate broad-spectrum inhibitor activity of the PCB. As with PCB, other phycobilins, such as phycourobilin (PUB), phycoerythrobilin (PEB), and phycoviolobilin (PVB) show similar binding affinity to SARS-CoV-2 Mpro and PLpro.

scholarly journals pH-Responsive Liposomes of Dioleoyl Phosphatidylethanolamine and Cholesteryl Hemisuccinate for the Enhanced Anticancer Efficacy of Cisplatin

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 129
Author(s):  
Hassan Shah ◽  
Asadullah Madni ◽  
Muhammad Muzamil Khan ◽  
Fiaz-ud-Din Ahmad ◽  
Nasrullah Jan ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Release Rate ◽  
In Vitro Release ◽  
Chemotherapeutic Agents ◽  
Ph Responsive ◽  
Scanning Calorimetry ◽  
Cholesteryl Hemisuccinate ◽  
Vitro Release

The current study aimed to develop pH-responsive cisplatin-loaded liposomes (CDDP@PLs) via the thin film hydration method. Formulations with varied ratios of dioleoyl phosphatidylethanolamine (DOPE) to cholesteryl hemisuccinate (CHEMS) were investigated to obtain the optimal particle size, zeta potential, entrapment efficiency, in vitro release profile, and stability. The particle size of the CDDP@PLs was in the range of 153.2 ± 3.08–206.4 ± 2.26 nm, zeta potential was −17.8 ± 1.26 to −24.6 ± 1.72, and PDI displayed an acceptable size distribution. Transmission electron microscopy revealed a spherical shape with ~200 nm size. Fourier transform infrared spectroscopic analysis showed the physicochemical stability of CDDP@PLs, and differential scanning calorimetry analysis showed the loss of the crystalline nature of cisplatin in liposomes. In vitro release study of CDDP@PLs at pH 7.4 depicted the lower release rate of cisplatin (less than 40%), and at a pH of 6.5, an almost 65% release rate was achieved compared to the release rate at pH 5.5 (more than 80%) showing the tumor-specific drug release. The cytotoxicity study showed the improved cytotoxicity of CDDP@PLs compared to cisplatin solution in MDA-MB-231 and SK-OV-3 cell lines, and fluorescence microscopy also showed enhanced cellular internalization. The acute toxicity study showed the safety and biocompatibility of the developed carrier system for the potential delivery of chemotherapeutic agents. These studies suggest that CDDP@PLs could be utilized as an efficient delivery system for the enhancement of therapeutic efficacy and to minimize the side effects of chemotherapy by releasing cisplatin at the tumor site.

scholarly journals α-Mangostin Hydrogel Film Based Chitosan–Alginate for Recurrent Aphthous Stomatitis

2019 ◽  
Vol 9 (23) ◽  
pp. 5235 ◽  
Author(s):  
Nasrul Wathoni ◽  
Nia Yuniarsih ◽  
Arief Cahyanto ◽  
Muhctaridi Muhctaridi
Keyword(s):  
In Vitro Release ◽  
Recurrent Aphthous Stomatitis ◽  
Aphthous Stomatitis ◽  
Fickian Diffusion ◽  
Garcinia Mangostana ◽  
Scanning Calorimetry ◽  
Main Compound ◽  
Discovery Studio ◽  
Hydrogel Film

Many antiseptic drugs, local anaesthetics, and corticosteroids have been used for effective therapy of recurrent aphthous stomatitis (RAS). However, these drugs have harmful side effects. α-mangostin (α-M), a main compound of mangosteen (Garcinia mangostana L.) peel, has been known as a wound healing agent. In addition, hydrogel film as dressings designed to separate mucosal lesions from the oral environment, and improve the effectiveness of RAS therapy. The purpose of this study was to develop α-M hydrogel film based chitosan–alginate (ChAlg/α-M HF) for RAS. The in silico study by Discovery studio visualizer and AutoDock confirmed that hydrogen bonding between Ch, Alg, and α-M occurred. The results of physicochemical characterizations by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) indicated that the ChAlg/α-M HF had a lower crystalline form compared to pure α-M. In addition, ChAlg/α-M HF significantly improved the swelling ratio and tensile strength compared to that of ChAlg HF. Moreover, the existence of Alg increased the degradability of Ch, and closely related to the release of α-M from ChAlg HF. The in vitro release study confirmed that the release of α-M from ChAlg/α-M HF was the Fickian diffusion model. Finally, the mucoadhesive study revealed that ChAlg/α-M HF had a good mucoadhesive property. These results suggest that hydrogel film-based chitosan–alginate have the potential as carriers of α-M for RAS therapy.

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF PSEUDOEPHEDRINE HCL

2020 ◽  
pp. 121-127
Author(s):  
SAMIULLAH ◽  
SYED UMER JAN ◽  
RAHMAN GUL ◽  
SYED JALALUDIN ◽  
ASMATHULLAH
Keyword(s):  
Castor Oil ◽  
In Vitro Release ◽  
Spectroscopic Studies ◽  
Tween 20 ◽  
Scanning Calorimetry ◽  
Eucalyptus Oil ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Xrd Studies

Objective: This study was conducted to design a transdermal dosage form of pseudoephedrine HCL and to evaluate its release under controlled rates for sustained transdermal delivery of Pseudoephedrine. Methods: Transdermal patches were prepared by the casting evaporation method. Utilizing eudragit RL100. Patches were characterized by physical appearance, moisture content, thickness, weight variation, folding endurance, tensile strength and stability studies. Fourier transform infrared spectroscopic studies (FTIR), differential scanning calorimetry analysis (SCA) and XRD studies. Four different permeation enhancer (Tween 20, thymus oil, castor oil and eucalyptus oil) was employed. In vitro release of drugs was done in the dissolution paddle apparatus. Release studies were performed in distilled water at 37 °C. Scanning electron microscope studies were performed before and after the drug. Results: Transdermal patches with enhancers were formulated successfully with a concentration of 1% (W/V). The patches indicated stable physicochemical characteristics. FTIR, SCA and XRD Studies showed that there were no physical and chemical interactions between excipients and drugs. Results of in vitro permeation studies showed that enhancers used in this study increased drug released. The enhancers showed faster released than no enhancer. This arrangement can be shown as Tween>Eucalyptus oil>Thymus oil and castor oil. Formulation F2 is optimized among all formulations showed an 83.3% release. Conclusion: Transdermal patches of pseudoephedrine were successfully developed by using pseudo epinephrine HCL. These patches proved to be very useful for therapeutic purposes in the pharmaceutical industry without making the patients unconscious, unlike the trivial methods of treatment.

scholarly journals Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

2020 ◽  
Vol 2020 ◽  
pp. 1-15
Author(s):  
Qiuchen Cheng ◽  
Wen Qin ◽  
Yanhong Yu ◽  
Guojian Li ◽  
Jizhou Wu ◽  
...  
Keyword(s):  
Smooth Muscle Actin ◽  
Drug Loading ◽  
In Vitro Release ◽  
Tween 80 ◽  
Original Method ◽  
Scanning Calorimetry ◽  
Experimental Conditions ◽  
Evaporation Method ◽  
Genistein Treatment

The objective of this study is to improve the bioavailability of genistein by encapsulation with polyethylene glycol-polylactic acid (PEG-PLA) copolymers. Genistein micelles (GMs) prepared using a modified emulsion-evaporation method were more stable than those made with the original method. The effect of polyvinyl alcohol, Tween 80, sonication time, PEG-PLA/genistein ratio, and organic phase (acetone)/H2O ratio on the size, polydispersity index, encapsulation efficiency, and drug loading efficiency of GMs was investigated. GMs were obtained and characterized under optimal experimental conditions. For long-term storage, GMs were lyophilized by freeze drying with trehalose to produce genistein lyophilized powder (GLP). The analysis of GLP by Fourier-transform infrared spectroscopy and differential scanning calorimetry showed that genistein was successfully incorporated into the micellar structure. In vitro release experiments revealed that the incorporation of genistein into PEG-PLA copolymers significantly improved its solubility and bioavailability. GLP was more potent in inhibiting the proliferation of HSC-T6 cells than genistein. Treatment with GLP at 10–20 μg/mL for 48 h significantly inhibited the protein expression of α-smooth muscle actin and collagen I in HSC-T6 cells compared with the control. These data demonstrated that the improved solubility and bioavailability of genistein in the form of GLP enhanced its antifibrotic effect in vitro.

FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES CONTAINING CAFFEINE TO TREAT CLINICAL MASTITIS

2020 ◽  
pp. 72-78
Author(s):  
AMRUTHA U ◽  
SUSHMITHA B ◽  
SHAIK RUBINA ◽  
PADMINI IRIVENTI
Keyword(s):  
Sustained Release ◽  
Solid Lipid Nanoparticles ◽  
Evaluation Studies ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Clinical Mastitis ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Solid Lipid

Objective: The objective of the present study was to formulate and evaluate caffeine loaded solid lipid nanoparticles (SLNs) in the treatment of clinical mastitis. Methodology: These were prepared by homogenization technique using cholesterol, tween 80, and chloroform as excipients. Preformulation studies such as ultraviolet spectrophotometry, Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC) were performed for the drug. Entrapment efficiency and in vitro dissolution studies were carried out for prepared SLN’s and the optimum formulation (F2) was taken for further studies such as FTIR, DSC, scanning electron microscopy, particle size, and zeta potential analysis. Results: Obtained results stated that prepared SLNs are roughly spherical in nature and are in nanorange. These were incorporated in Carbopol gel and further evaluation studies such as pH, spreadability, viscosity, homogeneity, and in vitro drug diffusion studies were carried out. All the results obtained state that prepared nanogel has shown sustained release of drug. The antimicrobial study was carried out using Staphylococcus aureus and it was confirmed by appearance of the zone of inhibition. Conclusion: Nanogel that contains Caffeine SLNs with 1:2 ratio drug:lipid has shown good in vitro release. Sustained release of Caffeine drug till 12 h was achieved by delivering it in the form of nanogel.

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