AN ASSESSMENT ON BUCCAL MUCOADHESIVE DRUG DELIVERY SYSTEM

Buccal drug delivery system (BDDS) has won a variety of exposure and traction as it possesses plenty of advantages and benefits as evaluate to different mucosal drug delivery systems. Buccal path for systemic drug delivery, the use of mucoadhesive polymers twill significantly increase the efficacy of many tablets, has been of outstanding interest over the previous couple of decades. This article affords a precise of BDDS mechanisms, consisting of a composition of the oral mucosa, delivery mechanism, numerous forms of BDDS, formulation, assessment and application of BDDS. Additionally, this text affords a precis over the patents, advertised products and destiny factors of BDDS. In this evaluation article, we've got tried to assemble the maximum significant reports (1988 to 2021) of formulation, assessment, application, patents of BDDS. This review will help pharmaceutical researchers to clarify the potential of BDDS to overcome the various existing drug delivery dispute like the efficiency of absorption, permeability and bioavailability of drugs

FORMULATION AND OPTIMIZATION AND IN VITRO CHARACTERIZATION OF OLANZAPINE LIPOSOME

Objective: Olanzapine (OZ) is a thioeno benzodiazepine class second-generation or atypical antipsychotic that selectively binds to central dopamine D2 and serotonin (5-HT2c) receptors used for the treatment of schizophrenia and bipolar disorder. The present paper is aimed at developing an optimized liposome-loaded OZ as an approach for brain targeting through the nasal route for effective therapeutic management of schizophrenia. Methods: The OZ liposomes were prepared by the thin-film hydration method. Various independent variable such as phospholipid, cholesterol and sonication time was optimized by using Design-Expert® Software to obtain the dependent variables of entrapment efficiency, vesicle size and zeta potential. The optimized formulation was predicted based on the response obtained by the point prediction method. Results: The entrapment efficiency of the formulation was range between 72.9 and 85.1 %. The average particle size of all the 15 experimental runs lies between the minimum and maximum values of the size 258.33 to 325.32 nm, respectively. The zeta potential ranges from-27.53 to-11.46 mV. The optimized formulation for characterized for its morphology by Transmission Electron Microscopy (TEM). In vitro release studies of OZ-loaded liposomal formulation was carried by dialysis sac method using pH 7.4 phosphate buffer (PBS) as a medium. The maximum release was found to be 98.43±1.2 % up to 24 h. The R2 zero-order kinetics and Korsmeyer-Peppas model was found to be 0.9919 and 0.9664, respectively. The zero-order shows the best-fit model with a highest R2 value exhibiting better correlation and the ‘n’ value was also found to be 0.85; indicating both diffusion-controlled and swelling-controlled drug release that is anomalous transport. Conclusion: The results, clearly states that the prepared formulations justify the parameters and OZ might be a suitable candidate to target the brain through nasal delivery

Moisture Dependent Physical Properties of Black gram

Physical properties of Black gram are important during harvesting, cleaning and drying with machines and also during improvement of these machines. This study was conducted to evaluate some moisture-dependent physical properties of Black gram namely, grain dimensions, thousand grain mass, surface area, sphericity, bulk density, true density, porosity and angle of repose. As the moisture content increased from 8.696% to 21.951% d.b., the three axial dimensions of the Black gram increased and the arithmetic and geometric mean diameter ranged from 3.736 ± 0.14 to 4.276 ± 0.14 mm and 3.797 ± 0.13 to 4.322 ± 0.13 mm respectively. The hundred grain mass of Black gram were 42.52 ± 1.03 and 48.18 ± 0.45 kg. The sphericity values of Black gram increased from 79.69% to 82.82%. The bulk and true densities values for Black gram decreased with increase in moisture content. The porosity and angle of repose of Black gram increased from 38.06 to 42.60% and 28.4 to 32.2° respectively with increase in moisture content from 8.696% to 21.951% d.b

Thin layer and deep bed drying basic theories and modelling: a review

A comprehensive review of the fundamental theories governing the drying process is presented. The development of models of drying of agricultural products for thin layer and deep bed drying are discussed. The factors affecting drying and the biochemical changes which happen during drying are listed. Importance of moisture diffusion and activation energy consumption for modeling and optimizing the drying processes are highlighted

Therapeutic implications of current Janus kinase inhibitors as anti-COVID agents: A review

Severe cases of COVID-19 are characterized by hyperinflammation induced by cytokine storm, ARDS leading to multiorgan failure and death. JAK-STAT signaling has been implicated in immunopathogenesis of COVID-19 infection under different stages such as viral entry, escaping innate immunity, replication, and subsequent inflammatory processes. Prompted by this fact and prior utilization as an immunomodulatory agent for several autoimmune, allergic, and inflammatory conditions, Jakinibs have been recognized as validated small molecules targeting the rapid release of proinflammatory cytokines, primarily IL-6, and GM-CSF. Various clinical trials are under investigation to evaluate Jakinibs as potential candidates for treating COVID-19. Till date, there is only one small molecule Jakinib known as baricitinib has received FDA-approval as a standalone immunomodulatory agent in treating critical COVID-19 patients. Though various meta-analyses have confirmed and validated the safety and efficacy of Jakinibs, further studies are required to understand the elaborated pathogenesis of COVID-19, duration of Jakinib treatment, and assess the combination therapeutic strategies. In this review, we highlighted JAK-STAT signalling in the pathogenesis of COVID-19 and clinically approved Jakinibs. Moreover, this review described substantially the promising use of Jakinibs and discussed their limitations in the context of COVID-19 therapy. Hence, this review article provides a concise, yet significant insight into the therapeutic implications of Jakinibs as potential anti-COVID agents which opens up a new horizon in the treatment of COVID-19, effectively

Integrating network pharmacology with molecular docking to rationalize the ethnomedicinal use of Alchornea laxiflora (Benth.) Pax & K. Hoffm. for efficient treatment of depression

Background: Alchornea laxiflora (Benth.) Pax & K. Hoffm. (A. laxiflora) has been indicated in traditional medicine to treat depression. However, scientific rationalization is still lacking. Hence, this study aimed to investigate the antidepressant potential of A. laxiflora using network pharmacology and molecular docking analysis.Materials and methods: The active compounds and potential targets of A. laxiflora and depression-related targets were retrieved from public databases, such as PubMed, PubChem, DisGeNET, GeneCards, OMIM, SwissTargetprediction, BindingDB, STRING, and DAVID. Essential bioactive compounds, potential targets, and signaling pathways were predicted using in silico analysis, including BA-TAR, PPI, BA-TAR-PATH network construction, and GO and KEGG pathway enrichment analysis. Later on, with molecular docking analysis, the interaction of essential bioactive compounds of A. laxiflora and predicted core targets of depression were verified.Results: The network pharmacology approach identified 15 active compounds, a total of 219 compound-related targets, and 14,574 depression-related targets with 200 intersecting targets between them. SRC, EGFR, PIK3R1, AKT1, and MAPK1 were the core targets, whereas 3-acetyloleanolic acid and 3-acetylursolic acid were the most active compounds of A. laxiflora with anti-depressant potential. GO functional enrichment analysis revealed 129 GO terms, including 82 biological processes, 14 cellular components, and 34 molecular function terms. KEGG pathway enrichment analysis yielded significantly enriched 108 signaling pathways. Out of them, PI3K-Akt and MAPK signaling pathways might have a key role in treating depression. Molecular docking analysis results exhibited that core targets of depression, such as SRC, EGFR, PIK3R1, AKT1, and MAPK1, bind stably with the analyzed bioactive compounds of A. laxiflora.Conclusion: The present study elucidates the bioactive compounds, potential targets, and pertinent mechanism of action of A. laxiflora in treating depression. A. laxiflora might exert an antidepressant effect by regulating PI3K-Akt and MAPK signaling pathways. However, further investigations are required to validate

Застосування статистичних інструментів для формулювання та оптимізації мукоадгезивних буккальних плівок карведилолу шляхом використання природних полімерів

The aim and objective of this study was to create mucoadhesive buccal films that contained the multipurpose medical carvedilol, which has a variety of medicinal uses. Materials and methods. The films were equipped using a solvent casting technique and concentrations of natural polymers, including Sweet basil, Lime Basil seeds and Purple basil mucilage. The influence of Carbopol 934 P, a selected natural polymer, was also investigated. The formulation variables were improved by the use of a factorial design of experiments and evaluated for their physico-chemical and in vitro evaluations. Result. These evaluations provided crucial insights into the properties of the buccal films. To evaluate the release profile and release kinetics of carvedilol from the films, in vitro drug release experiments were carried out in a phosphate buffer solution. Ex vivo permeation tests using fresh sheep buccal mucosa were performed to evaluate the drug's permeation through the buccal membrane. Samples were taken at regular intervals, and a UV Spectrophotometer was used for analysis. With a polymer solution concentration at level "3," formulation run R20 showed the best optimized buccal formulation. This formulation shows promise for further in vivo research. Conclusions. The results of this study offer important new evidence about the design and efficacy of mucoadhesive buccal films containing carvedilol. The optimization of formulation parameters and the assessment of physicochemical properties and drug release kinetics contribute to the progress of reproducible buccal filmsМетою та завданням цього дослідження було створення мукоадгезивних буккальних плівок, які містили багатоцільовий медичний карведилол, який має різноманітне медичне застосування. Матеріали та методи. Плівки були виготовлені з використанням техніки лиття з розчинника та концентрації природних полімерів, включаючи васильок духмяний (базилік огородній), насіння лаймового базиліка та слиз фіолетового базиліка. Також було досліджено вплив обраного природного полімеру - Carbopol 934 P. Змінні рецептури були вдосконалені за допомогою факторного плану експериментів і оцінені за допомогою фізико-хімічних та in vitro досліджень. Результати. Результати досліджень забезпечили вирішальне розуміння властивостей буккальних плівок. Щоб оцінити профіль вивільнення та кінетику вивільнення карведилолу з плівок, проводили експерименти з вивільнення препарату in vitro у фосфатному буферному розчині. Також було проведено тестування на проникнення ex vivo з використанням свіжої слизової оболонки щік вівці для оцінки проникнення препарату крізь буккальну мембрану. Зразки відбирали через регулярні проміжки часу, а для аналізу використовували УФ-спектрофотометр. З концентрацією розчину полімеру на рівні «3» цикл R20 показав найкращу оптимізовану буккальну композицію. Ця формула є перспективною для подальших досліджень in vivo. Висновки. Результати цього дослідження пропонують важливі нові докази щодо створення та ефективності мукоадгезивних буккальних плівок, що містять карведилол. Оптимізація параметрів рецептури та оцінка фізико-хімічних властивостей і кінетики вивільнення препарату сприяють розвитку відтворюваних буккальних пліво

Застосування статистичних інструментів для формулювання та оптимізації мукоадгезивних буккальних плівок карведилолу шляхом використання природних полімерів

The aim and objective of this study was to create mucoadhesive buccal films that contained the multipurpose medical carvedilol, which has a variety of medicinal uses. Materials and methods. The films were equipped using a solvent casting technique and concentrations of natural polymers, including Sweet basil, Lime Basil seeds and Purple basil mucilage. The influence of Carbopol 934 P, a selected natural polymer, was also investigated. The formulation variables were improved by the use of a factorial design of experiments and evaluated for their physico-chemical and in vitro evaluations. Result. These evaluations provided crucial insights into the properties of the buccal films. To evaluate the release profile and release kinetics of carvedilol from the films, in vitro drug release experiments were carried out in a phosphate buffer solution. Ex vivo permeation tests using fresh sheep buccal mucosa were performed to evaluate the drug's permeation through the buccal membrane. Samples were taken at regular intervals, and a UV Spectrophotometer was used for analysis. With a polymer solution concentration at level "3," formulation run R20 showed the best optimized buccal formulation. This formulation shows promise for further in vivo research. Conclusions. The results of this study offer important new evidence about the design and efficacy of mucoadhesive buccal films containing carvedilol. The optimization of formulation parameters and the assessment of physicochemical properties and drug release kinetics contribute to the progress of reproducible buccal filmsМетою та завданням цього дослідження було створення мукоадгезивних буккальних плівок, які містили багатоцільовий медичний карведилол, який має різноманітне медичне застосування. Матеріали та методи. Плівки були виготовлені з використанням техніки лиття з розчинника та концентрації природних полімерів, включаючи васильок духмяний (базилік огородній), насіння лаймового базиліка та слиз фіолетового базиліка. Також було досліджено вплив обраного природного полімеру - Carbopol 934 P. Змінні рецептури були вдосконалені за допомогою факторного плану експериментів і оцінені за допомогою фізико-хімічних та in vitro досліджень. Результати. Результати досліджень забезпечили вирішальне розуміння властивостей буккальних плівок. Щоб оцінити профіль вивільнення та кінетику вивільнення карведилолу з плівок, проводили експерименти з вивільнення препарату in vitro у фосфатному буферному розчині. Також було проведено тестування на проникнення ex vivo з використанням свіжої слизової оболонки щік вівці для оцінки проникнення препарату крізь буккальну мембрану. Зразки відбирали через регулярні проміжки часу, а для аналізу використовували УФ-спектрофотометр. З концентрацією розчину полімеру на рівні «3» цикл R20 показав найкращу оптимізовану буккальну композицію. Ця формула є перспективною для подальших досліджень in vivo. Висновки. Результати цього дослідження пропонують важливі нові докази щодо створення та ефективності мукоадгезивних буккальних плівок, що містять карведилол. Оптимізація параметрів рецептури та оцінка фізико-хімічних властивостей і кінетики вивільнення препарату сприяють розвитку відтворюваних буккальних пліво

Development and evaluation of novel-trans-buccoadhesive films of Famotidine

The present investigation highlights the novel trans-buccoadhesive films of Famotidine, an H2 receptor antagonist used as an anti-ulcerative agent. The buccal films were fabricated by solvent casting technique with different polymer combinations of hydroxypropyl methylcellulose, carbopol-934P and polyvinyl pyrrolidone. Drug–polymer interaction studies by Fourier transform infrared spectroscopy show that there is no significant interaction between drug and polymers. The fabricated films were evaluated for their physicochemical characters like weight, thickness, surface pH, percentage moisture absorption, percentage moisture loss, swelling percentage, folding endurance, water vapor transmission and drug content. Stability study of buccal films was performed in natural human saliva. Ex vivo permeation studies were conducted using fresh sheep buccal mucosa and buccoadhesive strength was calculated by modified balance method and showed sufficient strength in all the formulations. Good correlation was observed between the in vitro drug release and in vivo drug release, with a correlation coefficient of 0.995. Drug diffusion from buccal films showed apparently zero order kinetics and release mechanism was diffusion controlled after considerable swelling