Development of novel mucoadhesive gels containing nanoparticle for buccal administration of dexamethasone

Abstract This study aimed to develop promising and innovative mucoadhesive gel systems containing dexamethasone-loaded nanoparticle to increase the effectiveness of treatment for oral precancerous lesions and to reduce side effects. In this respect, a dexamethasone-loaded nanoparticle formulation was prepared by using emulsification/solvent evaporation method. The nanoparticle has high zeta potential (-10.3±0.5 mV), low particle size (218.42±2.1), low polydispersity index (0.070±0.014) and high encapsulation efficiency (95.018±2.982%). To improve the mucosal retention time, the dexamethasone-loaded nanoparticle was dispersed in mucoadhesive gel using gellan gum. The developed gels offered appropriate pH value, high drug content, suitable mechanical and mucoadhesive performance and appropriate viscosity for mucosal administration. All formulations exhibited plastic flow and typical gel-type mechanical spectra after the determined frequency value. The developed formulations exhibited extended drug release as intended for these systems. Cytotoxicity was tested by MTT assay in human epithelioid carcinoma cell (HeLa) in vitro. The MTT assay showed that the blank formulations were non-toxic to cells. It was observed that the bioactivity of the free dexamethasone was potentiated by mucoadhesive gels containing dexamethasone-loaded nanoparticle in HeLa cells. Results from this study indicate that mucoadhesive gels are effective for the local treatment of precancerous lesions. Our findings showed that the developed formulations were worthy of further studies.

Influence of additives on swelling and mucoadhesion properties of glyceryl monooleate liquid crystals

Abstract Liquid crystalline systems of glyceryl monooleate/water are used as drug delivery systems due to their complex structure that controls drug diffusion. Mucoadhesive properties of glyceryl monooleate suggest it can be used for buccal delivery. Using additives is a strategy to modify physical and chemical properties of liquid crystalline systems and optimize their performance as a drug delivery system. However, the presence of additives can significantly alter properties such as phase behavior, swelling and mucoadhesion. Our aim is to investigate the influence of additives on swelling and mucoadhesion of glyceryl monooleate-based liquid crystals, intending them to be used as buccal drug delivery systems. The systems were characterized regarding their mesophases, swelling rate, and mucoadhesion. All the systems studied were able to absorb water and presented mucoadhesion, which is interesting for the development of buccal drug delivery systems. Additives induced phase transitions and affected the swelling performance, while mucoadhesive properties were poorly affected. Propylene glycol increased water uptake, while oleic acid induced the phase transition to the hexagonal phase and reduced the swelling rate. The association of oleic acid (5%) and propylene glycol (10%) resulted in a cubic phase system with strong mucoadhesive properties that can be a potential drug carrier for buccal delivery.

Oral trans-mucosal dexmedetomidine for controlling of emergence agitation in children undergoing tonsillectomy: a randomized controlled trial / Dexmedetomidina transmucosa oral para controle da agitação ao despertar em crianças submetidas a amigdalectomia: ensaio clínico randomizado

Abstract Objectives: Emergence agitation is a negative behavior commonly recorded after pediatric tonsillectomy. We investigated the efficacy of preoperative premedication with oral transmucosal buccal dexmedetomidine on the incidence and severity of emergence agitation in preschool children undergoing tonsillectomy under sevoflurane anesthesia. Methods: Ninety patients aged (3-6 years), ASA I‒II were enrolled into three groups (n = 30) to receive oral transmucosal dexmedetomidine 0.5 µg.kg-1 (Group DEX I), 1 µg.kg-1 (Group DEX II) or saline placebo (Group C). Our primary endpoint was the Watcha agitation score at emergence in PACU. Secondary outcomes were preoperative sedation score, intraoperative hemodynamics, postoperative Objective Pain Scale (OPS) and adverse effects. Results: The patients' demographics, preoperative sedation scores and extubation time showed no difference between groups. Significant differences between groups in incidence and frequency distribution of each grade of Watcha score were evident at 5 minutes (p= 0.007), 10 minutes (p= 0.034), 30 minutes (p= 0.022), 45 minutes (p= 0.034) and 60 minutes (p= 0.026), postoperatively with significant differences between DEX I and II groups. DEX groups showed lower OPS scores at 5 minutes (p= 0.011), 10 minutes (p= 0.037) and 30 minutes (p= 0.044) after arrival at PACU, with no difference between DEX I and II groups. Patients in DEX II group exhibited lower intraoperative mean heart rate at 15 min (p= 0.020), and lower mean arterial pressure at 30 minutes, (p= 0.040), 45 minutes (p= 0.002) and 60 minutes (p= 0.006) with no significant differences between groups in other time points. Conclusion: This study demonstrates the clinical advantage and the simple technique of oral transmucosal DEX premedication for emergence agitation in preschool children undergoing tonsillectomy under sevoflurane anesthesia compared with saline placebo. Trial registration Clinical Trials.gov trial registry: NCT02720705.

Resumo Objetivos: A agitação ao despertar da anestesia é um comportamento negativo comumente registrado após amigdalectomia pediátrica. Avaliamos a eficácia da pré-medicação com dexmedetomidina via transmucosa oral no pré-operatório sobre a incidência e gravidade da agitação ao despertar em crianças pré-escolares submetidas à amigdalectomia sob anestesia com sevoflurano. Métodos: Noventa pacientes entre três e seis anos e estado físico ASA I-II foram incluídos em três grupos (n = 30) para receber 0,5 µg.kg-1 ou 1 µg.kg-1 de dexmedetomidina via transmucosa oral (Grupo DEX I e Grupo DEX II, respectivamente) ou solução salina (Grupo C). O desfecho primário foi o escore de agitação ao despertar medido com a escala de Watcha na SRPA. Os desfechos secundários foram escore de sedação pré-operatória, hemodinâmica intraoperatória, escore OPS (Objective Pain Scale) e efeitos adversos no pós-operatório. Resultados: A demografia dos pacientes, os escores de sedação pré-operatória e o tempo de extubação não apresentaram diferença entre os grupos. Diferenças significativas entre os grupos na distribuição da incidência e frequência de cada grau do escore de Watcha foram evidentes aos 5 minutos (p = 0,007), 10 minutos (p = 0,034), 30 minutos (p = 0,022), 45 minutos (p = 0,034) e 60 minutos (p = 0,026) no pós-operatório, com diferenças significativas entre os grupos DEX I e II. Os grupos DEX apresentaram escores OPS mais baixos aos 5 minutos (p = 0,011), 10 minutos (p = 0,037) e 30 minutos (p = 0,044) após a chegada à SRPA, sem diferença entre os grupos DEX I e II. Os pacientes do grupo DEX II apresentaram menor frequência cardíaca média aos 15 minutos de intraoperatório (p = 0,020) e menor pressão arterial média aos 30 minutos, (p = 0,040), 45 minutos (p = 0,002) e 60 minutos (p = 0,006), sem diferenças significativas entre os grupos em outros momentos. Conclusão: Este estudo demonstra a vantagem clínica e a técnica simples da pré-medicação com DEX por via transmucosa oral para agitação ao despertar em crianças pré-escolares submetidas à amigdalectomia sob anestesia com sevoflurano, comparado à solução salina. Registro do estudo: Clinical Trials.gov trial registry: NCT02720705.

Effect of Topical Erythropoietin (EPO) on palatal wound healing subsequent to Free Gingival Grafting (FGG)

Abstract Free gingival grafting, the most predictable technique to increase the keratinized gingiva, leaves an open wound on the palate and the resulting discomfort during the healing phase is a significant concern. This study was intended to evaluate the effect of topical erythropoietin on healing of the donor site. Twelve patients lacking an attached gingiva at two sites in the mandible were included. In the test group, 1 mL of gel containing erythropoietin at a concentration of 4,000 IU mL-1 was applied to the donor site, whereas the control group was treated with 2 mL of the gel alone. On the second day after surgery, the same procedure was repeated. H2O2 was used to evaluate the amount of epithelialization. Clinical healing was compared using photographs and direct examination. The EPO group showed significantly better keratinization only on day 21. Comparison of clinical healing based on direct examination revealed significantly better healing in the test group on day 28. Furthermore, inflammation in the test group was lower than in the control group on the same day. Topical application of EPO improves palatal wound healing during the third and fourth weeks after free gingival graft procedures.

Buccal fat pad in reconstruction of oral defects

An ablative surgical procedure in the oral cavity is curative for oral and maxillofacial pathologies, but simultaneously produces hard and soft tissue defects. These defects produce functional and psychological problems in the post operative period

The Objective of the present study was to evaluate the efficacy ofbuccalfatpad in reconstruction of intra-oral defects, elaborate the surgical technique used and also identify its post operative complications

A prospective study was conducted on patients with oral defects covered by Buccalfatpad between July 2008 and January 2016 in department of oral and maxillofacial surgery of Khyber College of Dentistry Peshawar. The variables of the study were, Age, gender, cause of surgery and location of intraoral defect. Patients were subsequently evaluated for signs of epithelialisation and Post operative complications

A total of 50 patients [33 males and 17 females] were recruited in the study. Male to female ratio of patients was 1.94: Land Mean age of 51.25 years SD + 12.94. The most common cause of intraoral defect was because of excisions of malignant tumors of oral mucosa and salivary glands. Maxilla was the most common site for the surgical defects observed. The epithelialisation process was completed in 3 weeks without any complications in 44 patients. However dehiscence of the graft was seen in 6 patients, yielding success rate of 88%. We also noted limited mouth opening in cases of retro molar area defects, but this problem was resolved with post operative physiotherapy

It was concluded that buccal fat pad is a convenient, feasible and quick method of reconstruction for sealing intraoral defects

Uso terapéutico de los antibióticos en el tratamiento periodontal: revisión de la literatura / Therapeutic use of antibiotics in periodontal treatment: a review of the literature

Las enfermedades periodontales son consecuencia de la acumulación de la placa dental. Las bacterias presentes en ella inician un proceso inflamatorio en los tejidos periodontales por medio de la liberación de toxinas bacterianas. El tratamiento indicado implica terapias mecánicas no quirúrgicas y quirúrgicas y, en algunos casos, terapia farmacológica. En pacientes que no responden a la terapia mecánica, los estudios sugieren el uso de terapias complementarias con antibióticos locales o sistémicos. En esos casos, es necesario el desarreglo previo de la placa dental adherida a la superficie radicular. Los antibióticos, junto con el raspado y alisado radicular (RAR) y el colgajo periodontal, son una alternativa de agentes terapéuticos, pues garantizan resultados satisfactorios en el tratamiento periodontal. El objetivo de esta revisión es analizar las propiedades de los antibióticos como agentes coadyuvantes de la terapia periodontal...

A novel dosage form for buccal administration of bupropion

Bupropion is an antidepressant used in the treatment of smoking. The purpose of this study was to prepare controlled-release hydrogel films for buccal administration of bupropion and investigate its physicochemical and cytotoxic properties. The films were prepared from ultrapure sodium carboxymethylcellulose, hydroxypropylmethylcellulose K4M, and medium-viscosity chitosan. Evaluation of film physicochemical characteristics was based on scanning electron microscopy, bupropion content, mechanical strength (burst strength, relaxation, resilience, and traction), and cytotoxicity. Bupropion content in bilayer films was 121 mg per 9 cm2. The presence of bupropion modified film mechanical strength, but did not compromise the use of this pharmaceutical form. As shown by the cytotoxicity results, films containing bupropion did not cause cellular damage. Bupropion administration in the form of hydrogel films is a potentially useful alternative in the treatment of smoking.

A bupropiona é um antidepressivo utilizado no tratamento do tabagismo. O objetivo deste trabalho foi a preparação de filmes hidrogelatinosos de liberação controlada para administração bucal de bupropiona. Os filmes foram preparados utilizando carboximetilcelulose sódica ultrapurificada, hidroxipropilmetilcelulose K4M e quitosana de média viscosidade. As características físico-químicas dos filmes foram avaliadas por microscopia eletrônica de varredura, teor de bupropiona, resistência mecânica (perfuração, relaxação, resiliência e tração) e citotoxicidade. Os resultados mostraram que os filmes em bicamada apresentaram teor de bupropiona de 121 mg por 9 cm2 de filme e que a bupropiona modifica a resistência mecânica dos filmes, sem, no entanto, inviabilizar o uso desta forma farmacêutica. Os estudos de citotoxicidade mostraram que as formulações dos filmes contendo bupropiona não causam dano celular. Este estudo mostrou que a bupropiona veiculada na forma de filme hidrogelatinoso pode ser uma alternativa útil no tratamento do tabagismo.

Formulation and evaluation of taste mask pellets of granisetron hydrochloride as oro dispersible tablet

Orally disintegrating systems have carved a niche amongst the oral drug delivery systems due to the highest compliance of the patients, especially the geriatrics and pediatrics. In addition, patients suffering from dysphagia, motion sickness, repeated emesis and mental disorders prefer these medications because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in these dosage forms. However, the requirements of formulating these dosage forms with mechanical strength sufficient to withstand the rigors of handling and capable of disintegrating within a few seconds on contact with saliva are inextricable. The purpose of this research was to mask the bitter taste of granisetron hydrochloride. To mask the taste Kollicoat(r) Smartseal 30D was used as coating polymer for pellet coating. The coated pellets of the drug was directly compressed with different superdisintegrant as AC-Di-Sol, Explotab and Kollidon CL in different concentration 5.0-7.5% w/w into an ODT. The prepared tablets were evaluated for hardness, friability, weight variation, wetting time, wet absorption ratio, in-vitro disintegration time and in vitro dissolution studies. Tablets exhibited quick disintegration characteristics with Kollidon CL in concentration 7.5% w/w i.e., within 20 seconds, which is characteristic of orally disintegrating dosage forms. More than 98% of drug was released from the formulations within 15 minutes. Formulations subjected to stability testing as per the ICH guidelines for 3 months, indicated stability with no change in taste, hardness, drug content, disintegration time and dissolution profiles. Thus, the results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated dosage forms in the oral cavity.

Sistemas de desintegração oral têm um nicho entre os sistemas de administração de medicamentos por via oral devido à maior aceitação dos pacientes, especialmente os de geriatria e pediatria. Além disso, pacientes que sofrem de disfagia, enjoo de movimento, emese repetida e distúrbios mentais preferem estes medicamentos porque não podem engolir grande quantidade de água. Além disso, os fármacos que exibem absorção satisfatória a partir da mucosa oral ou que se destinam a ação farmacológica imediata podem ser vantajosamente formulados nestas formas de dosagem. No entanto, a formulação destas formas farmacêuticas exige-lhes resistência mecânica suficiente para suportar os rigores do manuseio e capacidade de desintegrar dentro de alguns segundos em contato com a saliva. O objetivo desta pesquisa foi o de mascarar o gosto amargo de cloridrato de granisetrona. Para mascarar o sabor, utilizou-se Kollicoat smartseal 30D como polímero para io revestimento dos péletes. Os péletes revestidos do fármaco foram diretamente comprimidos com superdesintegrante diferente como Ac-Di-Sol, Explotab e Kollidon CL, em diferentes concentrações 5.0-7.5% m/m em comprimidos de dispersão oral (ODT). Os comprimidos preparados foram avaliados quanto à dureza, friabilidade, variação de peso, ao tempo de umedecimento, à razão de absorção de umidade, ao tempo de desintegração in vitro e em estudos de dissolução in vitro. Os comprimidos apresentaram características de desintegração rápida com Kollidon CL, em concentração de 7,5% m/m, ou seja, dentro de 20 segundos, o que é característico para formas farmacêuticas de desintegração oral. Mais do que 98% do fármaco foi liberado a partir das formulações no prazo de 15 minutos. Formulações submetidas a testes de estabilidade de acordo com as diretrizes da ICH por 3 meses indicaram estabilidade sem alteração no sabor, dureza, teor de fármaco, tempo de desintegração e perfis de dissolução. Assim, os resultados demonstraram que o mascaramento de gosto foi bem-sucedido e atingiu-se rápida desintegração das formas de dosagem na cavidade oral.

Cumplimiento de normas que rigen la administración de fármacos por el personal de enfermería en la Caja Nacional de Salud Cochabamba, segundo semestre del 2011 / Compliance with rules governing the administration of drugs by nurses in the National Health Fund Cochabamba, second half of 2011

La presente investigación tiene como objetivo general describir el cumplimiento de las normas que rigen la administración de fármacos por el personal de enfermería en la Caja Nacional de Salud de Cochabamba; en tal sentido, las normas de la administración de medicamentos forman parte de las funciones terapéuticas de enfermería que deben ser aplicadas constantemente para brindar una atención de calidad y con responsabilidad, sujetos al cuidado integral que asegure bienestar y seguridad del paciente. En la investigación se realizó un estudio de tipo descriptivo con una población de 20licenciadas de enfermería, de las cuales se obtuvo la muestra de forma aleatoria, a las que fue aplicado el instrumento que midió las variables en sus indicadores de cumplimiento y conocimiento de las normas para la administración de medicamentos, el análisis se hizo mediante estadísticas descriptivas. Los resultados obtenidos evidencian de forma general que el personal de enfermería tiene un conocimiento bueno en un 50%; sin embargo, en lo referente a la aplicación de las normas durante los procedimientos de administración de fármacos, los porcentajes son menores, siendo la más cumplida la relacionada con la dosis correcta

Mucoadhesive buccal patches of lornoxicam: II- in-vivo evaluation and clinical efficacy

Lornoxicam is a NSAID of the oxicam class and it has the same side effects of this group when taken orally. In attempts to avoid the systemic side effects of lornoxicam [e.g. gastric irritation] and to achieve sustained release of the drug, several buccal patch formulations containing lornoxicam were prepared using different polymers and were evaluated for in-vitro characteristics in part I of this study. In the current study, the selected formulations [based on the previous in-vitro data] are evaluated for in-vivo performance using experimental animals and clinical efficacy on human volunteers. Pharmacokinetic parameters were assessed following application of the selected patches in rabbits. A comparative clinical study was conducted on patients with post-operative pain and edema following maxillofacial operations. The results of the in-vivo animal experiment showed that lornoxicam formulated in different buccal patches was successfully delivered to the systemic circulation and showed high absolute bioavailability of lornoxicam. The clinical study results revealed that sodium carboxy methyl cellulose [NaCMC, 3%] formulation applied to the buccal mucosa was slightly better or equally effective to the orally administered commercial oxicam product [Feldene Flash tablets] in reducing pain level, swelling and tenderness within a period of 4 days with no observed side effects. These findings suggest that lornoxicam administered in this buccal patch may present a potential therapeutic use as a strong anti-inflammatory and analgesic agent

Preparation of fluconazole buccal tablet and influence of formulation expedients on its properties / 药学学报

The aim of present study was to prepare buccal tablets of fluconazole for oral candidiasis. The dosage forms were designed to release the drug above the minimum inhibitory concentration for prolonged period of time so as to reduce the frequency of administration and to overcome the side effects of systemic treatment. The buccal tablets were prepared by using Carbopol 71G and Noveon AA-1 by direct compression method. Microcrystalline cellulose was used as the filler and its effect was also studied. The prepared dosage forms were evaluated for physicochemical properties, in vitro release studies and mucoadhesive properties using sheep buccal mucosa as a model tissue. Tablets containing 50% of polymers (Carbopol & Noveon) were found to be the best with moderate swelling along with favorable bioadhesion force, residence time and in vitro drug release. The in vitro drug release studies revealed that drug released for 8 h, which in turn may reduce dosing frequency and improved patient compliance in oral candidiasis patients.

Farmacocinética e farmacodinâmica do misoprostol em Obstetrícia / Pharmacokinetics and pharmacodynamics of misoprostol in Obstetrics

Nos últimos anos a antecipação do parto vem sendo uma prática frequente na Obstetrícia. O misoprostol é um produto sintético, metil análogo da prostaglandina E1 que tem recebido maior atenção, principalmente para a indução do trabalho de parto e do abortamento, além de outras indicações, como controle da hemorragia pós-parto e para promover modificações na cérvice uterina, facilitando a realização de procedimentos como histeroscopia e colocação de dispositivo intrauterino. A administração do misoprostol atualmente é realizada por diferentes vias: oral, vaginal, bucal, sublingual e retal. Assim, é prudente o conhecimento da farmacologia, dos efeitos e mecanismos de ação do misoprostol nas diferentes formas de administração, com base nas evidências científicas e de acordo com os graus de recomendação. O maior pico do nível plasmático de misoprostol, em ordem decrescente, é do grupo sublingual, oral, vaginal com adição de água e vaginal. A biodisponibilidade é também maior na via sublingual. Entretanto, o nível plasmático é mantido por um maior período de tempo quando a via vaginal é utilizada.

Anticipation of delivery has been a frequent practice in Obstetrics nowadays. Misoprostol is a synthetic metyl analogue of prostaglandin E1 that has been used mainly for induction of labor and abortion, as well as for other indications like prevention and control of postpartum hemorrhage. In Gynecology, its use has been introduced to induce cervical modifications for facilitating gynecologic procedures as hysteroscopy and intrauterine device insertion. Misoprostol administration can be done by different routes: oral, vaginal, buccal, sublingual and rectal. Therefore, it is prudent to study pharmacokinetics and pharmacodynamics of this drug and its various routes of administration, according to scientific evidences and grades of recommendation. The highest plasmatic peak of misoprostol, in decreasing order, is sublingual, oral, vaginal and vaginal plus water administration route. Bioavailability is also greater for sublingual route. Notwithstanding, plasmatic levels are maintained for more time when vaginal route is used.

Design and in vivo evaluation of carvedilol buccal mucoadhesive patches

The buccal region offers an attractive route of administration for systemic drug delivery. Carvedilol [dose, 3.125-25 mg] is beta-adrenergic antagonist. Its oral bioavailability is 25-35% because of first pass metabolism. Buccal absorption studies of a carvedilol solution in human volunteers showed 32.86% drug absorption. FTIR and UV spectroscopic methods revealed that there was no interaction between carvedilol and polymers. Carvedilol patches were prepared using HPMC, carbopol 934, eudragit RS 100, and ethylcellulose. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH. In vitro release studies were conducted for carvedilol-loaded patches in phosphate buffer [pH, 6.6] solution. Patches exhibited drug release in the range of 86.26 to 98.32% in 90 min. Data of in vitro release from patches were fit to different equations and kinetic models to explain release profiles. Kinetic models used were zero and first-order equations, Hixon-Crowell, Higuchi, and Korsmeyer-Peppas models. In vivo drug release studies in rabbits showed 90.85% of drug release from HPMC-carbopol patch while it was 74.63 to 88.02% within 90 min in human volunteers. Good correlation among in vitro release and in vivo release of carvedilol was observed

Medicamentos utilizados por pacientes odontopediátricos e seu potencial cariogênico / Medicines used by pediatric dentistry patients and its cariogenic potential

O uso de medicamentos faz parte do quotidiano de muitas crianças que sofrem com problemas crônicos ou doenças agudas recorrentes. A grande maioria das drogas desenvolvidas para Pediatria têm em sua composição algum tipo de açúcar para o "mascaramento" do seu sabor; o que, embora torne o medicamento mais aceitável pelas crianças, pode acarretar efeitos danosos à sua saúde dental. O objetivo desta pesquisa foi verificar o percentual de crianças das Clínicas de Odontopediatria da Universidade Federal de Santa Maria (UFSM) sob uso de medicação sistêmica e avaliar seu potencial cariogênico. Os instrumentos de pesquisa foram um questionário aplicado aos pais (n=100), inspeção das bulas para verificação dos edulcorantes presentes na fórmula, com potencial de causar xerostomia e da posologia usual dos medicamentos, assim como verificação do pH endógeno por meio de pHmetro Quimis, modelo Q400-A. Dezesseis por cento das crianças estavam fazendo uso de alguma medicação no momento da pesquisa. Das 84% restantes, 43% utilizavam medicações com frequência ou haviam utilizado no último ano. Foi verificado que a maior parte das madicações analisadas continha sacarose em sua composição e o pH endógeno de todos os medicamentos foi ácido, sendo inferior ao pH crítico para desmineralização do esmalte em 75% deles. O único medicamento encontrado com potencial de causar xerostomia foi o Claritin. Médicos e dentistas devem conhecer o potencial cariogênico dos medicamentos, prescrever medicamentos livre de sacarose, encorajar os pais a utilizarem a medicação prescrita e orientar à escovação com dentifrício após sua administração.

Efeito de medicações intracanal em remanescentes pulpares murinos e fibroblastos humanos cultivados. Estudo histopatológico e de citotoxicidade / Effect of canal dressings on murine remmant dental pulps and human cultured fibroblasts. Histopathological and cytotoxicity analyses

A medicação intracanal em Endodontia visa o controle do processo inflamatório originado a partir do quadro patológico e agravado no decorrer da instrumentação. O corticosteróide associado a antibacterianos vem sendo amplamente empregado com esse propósito. O objetivo desse estudo foi comparar a reação biológica a esses medicamentos intracanal em ambos, remanescentes pulpares murinos e fibroblastos cultivados. Setenta e duas raízes de 18 ratos adultos da linhagem Wistar e uma linhagem celular de fibroblastos humanos foram usadas para análises histológicas e de citotoxicidade respectivamente. Os grupos experimentais foram: GI - NDP; GII - Otosporin®; GIII - Rifocort e GIV - Rinosoro®. Os medicamentos permaneceram no canal radicular por 3, 7 e 14 dias. Depois disso, os espécimes foram analisados histologicamente. A citotoxicidade foi analisada pelo método da exclusão de células coradas pelo azul de Trypan. A viabilidade celular foi analisada em 0, 6, 12 e 24 horas após o contato com as drogas. Os resultados na avaliação histológica evidenciaram a presença de necrose em diferentes extensões do remanescente pulpar de todos os espécimes. A maior parte espécimes com necrose total foi observada no grupo III. No tecido vital sempre apareceu algum elemento de inflamação aguda (hiperemia ou polimorfonucleares neutrófilos), bem como de crônica (células mononucleares). A viabilidade celular das culturas de todos os grupos foi menor que 67 por cento, mostrando um efeito citotóxico de todos os medicamentos testados. O grupo III apresentou as menores viabilidades celulares, no entanto, não houve diferença estatística entre as viabilidades dos grupos experimentais. Embora esse estudo tenha sido baseado em análise qualitativa pôde-se observar que o Rifocort mostrou ser mais agressivo para as polpas dentais in vivo e para os fibroblastos in vitro do que o NDP, o Otosporin® e o Rinosoro®.

Análise qualitativa e quantitativa da resposta inflamatória frente a diferentes medicações de uso endodôntico - Iodofórmio e hidróxido de cálcio - Quando aplicadas em tecido subcutâneo do dorso de rato / Qualitative and quantitative analysis of the inflamatory reaction promoted by diifferent endodontic dressnigs - calcium hydroxide and iodoformium - on the subcutaneous tissue of rats

O presente estudo teve por objetivo avaliar quantitativa e qualitativamente as reações que o organismo desenvolve em relação a duas drogas utilizadas como medicação intracanal - iodofórmio e hidróxido de cálcio -, quando as mesmas são implantadas em dorso de ratos. Para tanto foram utilizados vinte ratos albinos (Rattus norvegicus, var albino, linhagem Wistar), nos quais foram realizadas duas incisões no seu dorso onde foram inseridas, para um mesmo animal, a medicação a ser testada em seu veículo e consistência de uso clínico. Os grupos experimentais eram representados pelo grupo do tecido normal, íntegro (GCI), a ferida controle (GCII) onde nenhuma medicação foi colocada e os grupos tratados com iodofórmio (FOD) e hidróxido de cálcio (FOE). Passados períodos de três, cinco e onze dias, a região onde foi implantada a medicação era removida em bloco com o tecido adjacente. Neste momento a condição macroscópica era observada. Os fragmentos eram levados para fixação em Bouin e processados para análise histológica com a coloração H-E e tricrômico de Mason. Os mesmos eram submetidos a análise qualitativa e quantitativa. Neste caso através da avaliação de fotomicrografias com 550X de aumento de campos representativos do subcutâneo que deveriam ser divididas em 100 pontos com uma grade onde as estruturas mais representativas deveriam ser contadas seguindo a seguinte denominação: células epiteliais, fibras colágenas, fibroblastos, macrófagos, linfócitos, neutrófilos, vasos e outras estruturas (áreas de necrose, fibrócitos, folículos pilosos, espaços...

Preparation of buspirone hydrochloride buccal adhesive tablet and study on its drug release mechanism / 药学学报

<p><b>AIM</b>To prepare buspirone hydrochloride buccal adhesive tablet and investigate factors that influence drug release behavior and the drug release mechanism.</p><p><b>METHODS</b>Buspirone hydrochloride buccal adhesive tablet was prepared with double layers structure composed of drug core and adhesive layer. The materials of the drug core were carbopol 974 and lactose, the adhesive layers were carbopol 974 and HPMC K4M. The influence of drug release factors such as adhesive layer component, adhesive layer weight and adhesive tablet hardness was investigated. The relationship between adhesive layer weight and drug release mechanism in vitro was studied.</p><p><b>RESULTS</b>The results showed that the weight of the adhesive layer and the hardness of adhesive tablet showed significant effects on drug release, but the adhesive layer component showed no significant effect. The optimum prescription of buspirone hydrochloride buccal adhesive tablet was carbopol: HPMC = 1:1, adhesive layer weight = 50%, and adhesive tablet hardness = 4 kg. The study of drug release mechanism from adhesive tablet showed that it was double directions when adhesive layer weight was 20%, and single direction first then double directions when 33.33%, and single direction all along when 50%.</p><p><b>CONCLUSION</b>The speed and direction of drug release from adhesive tablet can be controlled by regulating adhesive layer weight.</p>