scholarly journals HPV Lesions and Other Issues in the Oral Cavity Treatment and Removal without Pain

2021 ◽  
Vol 22 (20) ◽  
pp. 11158
Author(s):  
Salima El Moussaoui ◽  
Mireia Mallandrich ◽  
Núria Garrós ◽  
Ana Cristina Calpena ◽  
Maria José Rodríguez Lagunas ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Well Being ◽  
In Vitro Test ◽  
Ketorolac Tromethamine ◽  
Applied Dose ◽  
Permeation Studies ◽  
And Control ◽  
High Degree

Due to different oral and dental conditions, oral mucosa lesions such as those caused by the human papilloma virus and temporomandibular joint pathologies often have to be treated by surgical, ablative or extractive procedures. The treatment and control of pain and inflammation during these procedures is essential to guarantee the patient’s well-being. For the foregoing reason, a hydrogel based on sodium alginate and hyaluronic acid containing 2% of ketorolac tromethamine has been developed. We characterized it physically, mechanically and morphologically. The rheological results suggest that the formulation can be easily and gently applied. Ex vivo permeation studies show that Ketorolac Tromethamine is able to penetrate through the buccal and sublingual mucosae, in addition to being retained in the mucosae’s structure. Through an in vitro test, we were able to evaluate the role that saliva plays in the bioavailability of the drug, observing that more than half of the applied dose is eliminated in an hour. The histological and cytotoxic studies performed on pigs in vivo showed the excellent safety profile of the formulation, as well as its high tolerability. In parallel, a biomimetic artificial membrane (PermeaPad®) was evaluated, and it showed a high degree of correlation with the oral and sublingual mucosa.

scholarly journals Formulation and evaluation of buccoadhesive quetiapine fumarate tablets

2012 ◽  
Vol 48 (2) ◽  
pp. 335-345 ◽  
Author(s):  
Appa Rao Potu ◽  
Naresh Pujari ◽  
Shashidher Burra ◽  
Prabhakar Reddy Veerareddy
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Sodium Deoxycholate ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Quetiapine Fumarate ◽  
Zero Order Kinetics ◽  
Permeation Studies

The aim of present study was to develop and evaluate buccoadhesive Quetiapine Fumarate (QF) tablets, which is extensively metabolised by liver. Buccoadhesive tablets of QF were prepared using HPMC K4M, HPMC K15M and combination of carbopol and HPC as mucoadhesive polymers by direct compression method. Sodium deoxycholate was added to formulation to improve the permeation of drug. The formulations were tested for bioadhesion strength, ex vivo residence time, swelling time and in vitro dissolution studies and ex vivo permeation studies. Optimized formulation (F3) showed 92% in vitro release in 8 h and 67% permeation of drug through porcine buccal mucosa and followed fickian release mechanism with zero order kinetics. FTIR studies of optimized formulation showed no evidence of interaction between the drug and polymers. In vivo mucoadhesive behaviour of optimized formulation was performed and subjective parameters were evaluated.

scholarly journals Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel

Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 577 ◽  
Author(s):  
Wafaa E. Soliman ◽  
Tamer M. Shehata ◽  
Maged E. Mohamed ◽  
Nancy S. Younis ◽  
Heba S. Elsewedy
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Delivery Methods ◽  
Anti Cancer ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.

scholarly journals Formulation Development of Sublingual Cyclobenzaprine Tablets Empowered by Standardized and Physiologically Relevant Ex Vivo Permeation Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1409
Author(s):  
Haidara Majid ◽  
Andreas Puzik ◽  
Tanja Maier ◽  
Raphaela Merk ◽  
Anke Bartel ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vivo Studies ◽  
Process Automation ◽  
Formulation Development ◽  
Tissue Integrity ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
The Impact

Suitable ex vivo models are required as predictive tools of oromucosal permeability between in vitro characterizations and in vivo studies in order to support the development of novel intraoral formulations. To counter a lack of clinical relevance and observed method heterogenicity, a standardized, controlled and physiologically relevant ex vivo permeation model was established. This model combined the Kerski diffusion cell, process automation, novel assays for tissue integrity and viability, and sensitive LC-MS/MS analysis. The study aimed to assess the effectiveness of the permeation model in the sublingual formulation development of cyclobenzaprine, a promising agent for the treatment of psychological disorders. A 4.68-fold enhancement was achieved through permeation model-led focused formulation development. Here, findings from the preformulation with regard to pH and microenvironment-modulating excipients proved supportive. Moreover, monitoring of drug metabolism during transmucosal permeation was incorporated into the model. In addition, it was feasible to assess the impact of dosage form alterations under stress conditions, with the detection of a 33.85% lower permeation due to salt disproportionation. Integrating the coherent processes of disintegration, dissolution, permeation, and metabolization within a physiological study design, the model enabled successful formulation development for cyclobenzaprine sublingual tablets and targeted development of patient-oriented drugs for the oral cavity.

scholarly journals Preparation of Carbopol 934 Based Ketorolac Tromethamine Buccal Mucoadhesive Film: In Vitro, Ex Vivo, and In Vivo Assessments

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
M. Yasmin Begum ◽  
Ali Alqahtani ◽  
Mohammed Ghazwani ◽  
M. M. Ramakrishna ◽  
Umme Hani ◽  
...  
Keyword(s):  
Sodium Alginate ◽  
Residence Time ◽  
Ex Vivo ◽  
Ketorolac Tromethamine ◽  
Surface Ph ◽  
Folding Endurance ◽  
Anti Inflammatory ◽  
Pvp K30

The goal of present investigation was to formulate and evaluate ketorolac tromethamine (KTM) mucoadhesive buccal films. The films were prepared by solvent evaporation method using PVP K30, HPMC K4M, HPMC K15M, carbopol 934, chitosan, and sodium alginate as polymers and propylene glycol as plasticizer. The films were evaluated for thickness, weight variation, folding endurance, surface pH, swelling index, in vitro residence time, in vitro diffusion, release kinetics, ex vivo permeation, in vitro-ex vivo correlation, and in vivo pharmacological activities such as anti-inflammatory and analgesic activity. Thickness, weight, drug content, and folding endurance were found to be uniform for the films. Surface pH was 6.85 ± 0.10 , and swelling index was the highest ( 27.27 ± 0.37 ) for the best film containing carbopol 934 along with sodium alginate and PVP K 30 (formulation code F2). In vitro residence time was greater than 5 h, and in vitro % drug release was 98.71% for F2. It exhibited 55.49% of swelling inhibition at 5 h, and above 38.88% was maintained at even 8 h. The film F2 has shown maximum analgesic response of 17 sec at 5 h, and the response of 11 sec was maintained at even 8 h. The anti-inflammatory and analgesic effect of F2 was found be maximum while sustaining the effect for prolonged period when compared to free drug solution. Thus, KTM mucoadhesive buccal film containing carbopol 934, sodium alginate, and PVP K30 could be an effective alternative for conventional therapy with improved efficacy.

scholarly journals Formulation and in Vitro, ex Vivo and in Vivo Evaluation of Elastic Liposomes for Transdermal Delivery of Ketorolac Tromethamine

Pharmaceutics ◽  
2011 ◽  
Vol 3 (4) ◽  
pp. 954-970 ◽  
Author(s):  
Guadalupe Nava ◽  
Elizabeth Piñón ◽  
Luis Mendoza ◽  
Néstor Mendoza ◽  
David Quintanar ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Ex Vivo ◽  
Ketorolac Tromethamine ◽  
In Vivo Evaluation

Effects Of Bay g 6575 On Platelets And On Vascular PGI2 Production

1981 ◽  
Author(s):  
D E MacIntyre ◽  
E W Salzman
Keyword(s):  
Vascular Tissue ◽  
Ex Vivo ◽  
Platelet Rich Plasma ◽  
Duration Of Action ◽  
Antithrombotic Activity ◽  
Vascular Rings ◽  
And Control ◽  
Induced Aggregation

Bay g 6575 (1-[2-(β-naphthyloxy) ethyl]-3-methy1-2-pyrazolin-5-one) exerts a protective effect in several animal models of thrombosis. To elucidate its mechanism of action, we examined the effects of Bay g 6575 on platelets and on vascular PGI2 production. In vitro addition of Bay g 6575 (200 μM) to human citrated platelet rich plasma (PRP) did not inhibit aggregation induced by ADP or U44069, or augment inhibition of ADP-induced aggregation by PGD2, PGE1, PGI2 or papaverine. When added to isolated human or rat vascular rings, Bay g 6575 (200 μM) did not stimulate production of PGI2 or 6-oxo-PGF1α. Ex vivo studies one hour after administration of Baya g 6575 to rabbits (10 mg/kg, i.a.) or rats (100 mg/kg, p.o.) revealed no inhibition of ADP-induced aggregation or enhancement of the level of “circulating” PGI2 as measured by bio-immunoassay. When production of anti-aggregating activity by vascular rings from Bay g 6575 treated (B) and Control (C) rats were compared, in 6 of 8 experiments B inhibited more than C and B produced more 6-oxo-PGF1α than C (mean increase in B ± s.d.=74.3 ± 35.7%, range 42-135%). Production of antiaggregatory activity by “exhausted” C rings was enhanced by B>C platelet free plasma. In all cases, the inhibitor of aggregation produced by B and C rings acted on both human and rat PRP, and its effects could be reversed by anti-PGI1 antibodies that neutralize PGI2>6-oxo-PGE1>PGD2. When exogenous PGI2 was incubated with (exhausted) aspirin treated vascular rings, the duration of action of PGI2 was longer in the presence of B rings than C rings.Bay g 6575 has no direct effects on platelets or on vascular tissue. Its antithrombotic activity appears to be caused by regulation of PGI2 synthesis and metabolism, an effect mediated by factors, possibly Bay g 6575 metabolites, present in plasma after in vivo administration.

scholarly journals NOVEL NANOPARTICLES FOR THE ORAL DELIVERY OF LOW MOLECULAR WEIGHT HEPARIN: IN VITRO AND IN VIVO ASSESSMENT

2017 ◽  
Vol 10 (2) ◽  
pp. 254 ◽  
Author(s):  
Nallaguntla Lavanya ◽  
Indira Muzib ◽  
Aukunuru Jithan ◽  
Balekari Umamahesh
Keyword(s):  
Molecular Weight ◽  
Low Molecular Weight Heparin ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Low Molecular Weight ◽  
Scanning Calorimetry ◽  
Ex Vivo Permeation ◽  
Permeation Studies

Objective: The objective of the present study was to prepare and evaluate a novel oral formulation of nanoparticles for the systemic delivery of low molecular weight heparin (LMWH). Methods: Nanoparticles were prepared by polyelectrolyte complexation (PEC) method using polymers sodium alginate and chitosan. Entrapment efficiency of LMWH in nanoparticles was found to be  ̴88%. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X‑ray diffraction (XRD), Scanning electron microscopy (SEM)  studies carried for nanoparticles. In vitro release studies were performed for the formulations. Ex vivo permeation studies were performed optimized formulation by using small intestine of rat and in vivo studies were conducted on rat model.Results: In vitro release studies demonstrated that the release of LMWH was negligible in the stomach and high in the small intestine. FTIR has indicated that there is no interaction between the ingredients in nanoparticle. DSC and XRD studies confirmed that the amino groups of chitosan interacted with the carboxylic groups of alginate. Invitro % drug release of 95% was shown by formulation AC5. Ex vivo permeation studies have elucidated that ̴ 73% of LMWH was transported across the epithelium. Nanoparticles have shown enhanced oral bioavailability of LMWH as revealed by 4.5 fold increase in AUC of plasma drug concentration time curve.Conclusion: The results suggest that the nanoparticles prepared can result in targeted delivery of LMWH into systemic circulation via intestinal and colon routes. Novel nanoparticles thus prepared in this study can be considered as a promising delivery system.Keywords: Antifactor Xa activity, Chitosan, Differential scanning calorimetry, Sodium alginate, Low-molecular-weight heparin, Oral bioavailability.

scholarly journals Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress

Blood ◽  
2006 ◽  
Vol 109 (6) ◽  
pp. 2579-2588 ◽  
Author(s):  
Crescent R. Isham ◽  
Jennifer D. Tibodeau ◽  
Wendy Jin ◽  
Ruifang Xu ◽  
Michael M. Timm ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
B Cells ◽  
Cell Lines ◽  
Ex Vivo ◽  
Myeloma Cell ◽  
Lymphocytic Leukemia ◽  
Myeloma Cells ◽  
High Degree

Abstract Chaetocin, a thiodioxopiperazine natural product previously unreported to have anticancer effects, was found to have potent antimyeloma activity in IL-6–dependent and –independent myeloma cell lines in freshly collected sorted and unsorted patient CD138+ myeloma cells and in vivo. Chaetocin largely spares matched normal CD138− patient bone marrow leukocytes, normal B cells, and neoplastic B-CLL (chronic lymphocytic leukemia) cells, indicating a high degree of selectivity even in closely lineage-related B cells. Furthermore, chaetocin displays superior ex vivo antimyeloma activity and selectivity than doxorubicin and dexamethasone, and dexamethasone- or doxorubicin-resistant myeloma cell lines are largely non–cross-resistant to chaetocin. Mechanistically, chaetocin is dramatically accumulated in cancer cells via a process inhibited by glutathione and requiring intact/unreduced disulfides for uptake. Once inside the cell, its anticancer activity appears mediated primarily through the imposition of oxidative stress and consequent apoptosis induction. Moreover, the selective antimyeloma effects of chaetocin appear not to reflect differential intracellular accumulation of chaetocin but, instead, heightened sensitivity of myeloma cells to the cytotoxic effects of imposed oxidative stress. Considered collectively, chaetocin appears to represent a promising agent for further study as a potential antimyeloma therapeutic.

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