Comparative Evaluation of Efficacy and Safety of Herbal Preparation vis-a-vis Beclomethasone Cream on Radiation Induced Skin Injury in Head and Neck Carcinoma Patients Receiving Radiotherapy or Chemoradiation in Oncology Department at a Tertiary Care Hospital

Introduction: Radiation mitigators are the compounds whichcan minimize or ameliorate post irradiation-toxicity providedthey are administered before the onset of toxic symptoms.Hence, there is an urgent need to prevent harmful effectssecondary to ionizing radiations.Material and Methods: Sixty patients of Head and neckcarcinoma more than 18 years of age of either sex and willingto give informed consent were included in the study. In Group1, 30 patients received the Beclomethasone cream that wastopically applied from the day-1 of radiotherapy till 4-weeksafter completion of radiotherapy, whereas In Group-2, 30patients received the local application of the herbal paste fromthe day-1 of radiotherapy till 4-weeks after completion ofradiotherapy.Results: For measuring radiation-induced reactions, nonparametric test like chi-square test was applied and number ofpatients in different grades was calculated as per RTOGcriteria. Similarly for measuring radiation-induced mucosalreactions, chi-square test was applied and number of patientsin different grades was calculated as per RTOG-criteria.Conclusion: Present study revealed a marked beneficialeffects of herbal paste containing Azadirachta indica, aloevera, Ocimum sanctum and Curcuma longa on radiationinduced skin injury in patients with Head and neck carcinomaas compared to topical Beclomethasone cream.

Comparative Evaluation of Quality of Life in Patients of Head and Neck Carcinoma withRadiation Induced Skin-injury in Oncology Department at Tertiary Care Hospital

Radiation mitigators are the compounds which can minimize post irradiation-toxicity provided theyare administered before the onset of toxic symptoms. In present study we compared pre and posttreatment quality of life in head and neck cancer patients receiving radiotherapy.Sixty patients ofHead and neck carcinoma more than 18 years of age of either sex and willing to give informedconsent were included in the study. In Group-1, 30 patients received the Beclomethasone cream thatwas topically applied from the day-1 of radiotherapy till 4-weeks after completion of radiotherapy,whereas In Group-2, 30 patients received the local application of the herbal paste from the day-1 ofradiotherapy till 4-weeks after completion of radiotherapy. These 60 patients were evaluated at 6month post-therapy using the European organisation for research and treatment of cancer quality oflife questionnaire C30 .For measuring radiation-induced reactions, chi-square test was applied andnumber of patients in different grades was calculated as per Radiotherapy oncology group criteria.Similarly for measuring radiation-induced mucosal reactions, non-parametric test i.e chi-square testwas applied and number of patients in different grades was calculated as per radiotherapy oncologygroup criteria. As per quality of life questionnaire, evaluation on symptom scale revealed that fatigue,pain, dyspnoea, appetite loss and insomnia got worsened in Gp-1 patients, except for diarrhoea,constipation and nausea or vomiting while in Gp-2 patients, all symptoms showed improvement after6 month of completion of treatment. Comparing pre and post-treatment , the global health statusshowed statistically significant improvement in group-2 patients receiving polyherbal paste .The International Journal of Interdisciplinary and Multidisciplinary Studies (IJIMS), 2019, Vol 6, No.1,65-79. 66present study revealed a beneficial effects of polyherbal paste containing Azadirachta indica, aloevera, Ocimum sanctum and Curcuma longa on radiation induced skin injury in patients with Head andneck carcinoma as compared to topical Beclomethasone cream. Also there was improvement inquality of life in cancer patients receiving herbal paste measured at 6 month post-treatment.

Clinical Efficacy of Beclomethasone Dipropionate in Korean Patients with Ulcerative Colitis

PURPOSE: Our aim was to evaluate the efficacy and safety of oral beclomethasone dipropionate (BDP) in Korean patients with ulcerative colitis (UC). MATERIALS AND METHODS: The medical records of patients with active UC who were treated with BDP were retrospectively reviewed. Partial Mayo Clinic score (pMS) was calculated to determine disease activity. After 4 weeks of therapy, clinical remission, clinical response, and response failure rates were evaluated. Clinical remission was defined as a post-treatment pMS of 0 or 1, clinical response as a decrease of two of three points in pMS and >30% from baseline, and response failure as a lack of clinical response. Also, we considered that clinical remission was included in clinical response. RESULTS: Between July 2013 and April 2015, 95 patients with UC received BDP therapy at our institution (median age, 44 years; range, 12–81 years). After 4 weeks of therapy, clinical remission and clinical response rates were 50.5% and 73.7%, respectively. Mean change of pMS before and after BDP therapy was 2.4. There was no significant side effect reported. In multivariate analysis, disease activity was the only factor associated with a favorable response. Clinical remission rate was significantly higher in the mild disease activity group (66.7%) than that in the moderate or severe disease activity group (41.9%) (p=0.024). CONCLUSION: BDP is efficacious in inducing a clinical response or remission in Korean patients with UC. Patients with mild UC were more likely to be in remission than those with moderate or severe UC after receiving BDP for 4 weeks. BDP exhibited a good safety profile.

Pullulan as a stabilizer agent of polymeric nanocapsules for drug delivery

ABSTRACT Polymeric stabilizers have received attention in the preparation of nanostructured systems due to their ability to enhance formulation stability. Considering this, the objective of this work was to prepare poly(ε-caprolactone) nanocapsules using the pullulan as a polymeric stabilizer. The nanocapsules were prepared using the interfacial deposition method of preformed polymers and they were characterized in terms of pH, average diameter, polydispersity index, zeta potential, beclomethasone dipropionate content, encapsulation efficiency, photostability and drug release profiles. The formulations showed physicochemical characteristics consistent with nanocarriers for drug delivery such as: average diameter lower than 270 nm, polydispersity indexes lower than 0.2, negative zeta potential (-22.7 to -26.3 mV) and encapsulation efficiencies close to 100%. In addition, the nanocapsules were able to delay the beclomethasone dipropionate photodegradation under UVC radiation and by the dialysis bag diffusion technique, the nanocapsules were able to prolong the drug release. Thus, pullulan could be considered an interesting excipient to formulate polymeric nanocapsules.

Stability-indicating RP-HPLC method for determination of beclomethasone dipropionate in nanocapsule suspensions

abstract A simple stability-indicating RP-HPLC/UV method was validated for determination of beclomethasone dipropionate (BD) in nanocapsule suspensions. Chromatographic conditions consisted of a RP C18column (250 mm x 4.60 mm, 5 µm, 110 Å), using methanol and water (85:15 v/v) as mobile phase at 1.0 mL/min with UV detection at 254 nm. The calibration curve was found to be linear in the concentration range of 5.0-25.0 µg/mL with a correlation coefficient > 0.999. Precision was demonstrated by a relative standard deviation lower than 2.0%. Accuracy was assessed by the recovery test of BD from nanocapsules (98.03% to 100.35%). Specificity showed no interference from the components of nanocapsules or from the degradation products derived from acid, basic and photolytic conditions. In conclusion, the method is suitable to be applied to assay BD in bulk drug and in nanocapsules, and it can be employed to study stability and degradation kinetics.

resumo Um método simples de CLAE-FR/UV indicativo de estabilidade foi validado para a determinação do dipropionato de beclometasona (BD) em suspensões de nanocápsulas. As condições cromatográficas foram: coluna C18 fase reversa (250 mm x 4,60 mm, 5 µm, 110 Å), usando como fase móvel metanol e água (85:15 v/v) a 1,0 mL/min, com detecção UV a 254 nm. A curva de calibração foi linear no intervalo de 5,0-25,0 µg/mL com coeficiente de correlação >0,999. A precisão foi demonstrada por um desvio padrão relativo menor que 2,0%. A exatidão foi avaliada pelo teste de recuperação do BD a partir das nanocápsulas (98,03% a 100,35%). O teste de especificidade não mostrou interferência dos componentes das nanocápsulas e nem dos produtos de degradação derivados de condições ácidas, básicas e fotolíticas. Em conclusão, o método é adequado para ser aplicado na avaliação do BD puro e em nanocápsulas e pode ser empregado para o estudo de estabilidade e degradação cinética.

Microbial biotransformation of beclomethasone dipropionate by Aspergillus niger

In the present research, the steroidal anti-asthmatic drug beclomethasone dipropionate was subjected to microbial biotransformation by Aspergillus niger. Beclomethasone dipropionate was transformed into various metabolites first time from microbial transformation. New drug metabolites produced can act as new potential drug molecules and can replace the old drugs in terms of safety, efficacy, and least resistance. They were purified by preparative thin layer chromatography technique, and their structures were elucidated using modern spectroscopic techniques, such as 13C NMR, 1H NMR, HMQC, HMQC, COSY, and NOESY, and mass spectrometry, such as EI-MS. Four metabolites were purified: (i) beclomethasone 17-monopropionate, (ii) beclomethasone 21-monopropionate, (iii) beclomethasone, and (iv) 9beta,11beta-epoxy-17,21-dihydroxy-16beta-methylpregna-1,4-diene-3,20-dione 21-propionate.

Na pesquisa presente o fármaco esteróide antiasmático dipropionato de beclometasona foi submetido à biotransformação microbiana pelo Aspergillus niger. O dipropionato de beclometasona foi transformado, pela primeira vez, em metabólitos variados por biotransformação microbiana. Novos metabólitos do fármaco produzidos podem agir como novas moléculas potenciais e podem substituir os fármacos antigos em questão de segurança, eficácia e mínima resistência. Eles foram purificados por cromatografia em camada delgada preparativa e as suas estruturas foram elucidadas usando técnicas espectroscópicas modernas, como 13C NMR, 1H NMR; HMQC; HMQC; COSY, NOESY e espectrometria de massas, por exemplo, EI-MS. Purificaram-se quatro metabólitos, denominados (i) 17-monopropionato de beclometasona; (ii) 21-monopropionato de beclometasona: (iii) beclometasona e (iv) 21-propionato de 9beta,11beta-epoxi-17,21-diidroxi-16beta-metilpregna-1,4-dieno-3,20-diona.

Formulation and evaluation of CFC free inhalers for beclomethasone dipropionate

Beclomethasone dipropionate CFC free inhalation formulations were developed with a view to treat asthma prophylactically. Dry powder inhalers (DPI) for beclomethasone dipropionate were prepared with different grades of lactose monohydrate. The influence of carrier and overages on performance of DPI was studied. Metered dose inhalers (MDI) with HFA based propellants were formulated with various doses, overages and different concentrations of alcohol. Formulated DPI and MDI were evaluated for various official and unofficial quality control tests. The influence of over doses on valve delivery, effect of overages on emitted dose and influence of alcohol on spray pattern from MDI were studied. The better fine particle fraction and emitted dose were obtained from the DPI formulated with 10:90 ratio of fine lactose: coarse lactose and with 20% w/w overages. The studies on MDI revealed that the 15% of overdoses are required for effective valve delivery and 20% overages are required for 100% drug delivery. 5-10%v/v alcohol was found to be preferable to get optimum emitted dose and fine particle fraction.

Desenvolveram-se formulações por inalação de dipropionato de beclometasona, livres de CFC, com o objetivo de tratar a asma profilaticamente. Prepararam-se inaladores de pó seco (DPI) para o dipropionato de beclometasona com diferentes gradações de lactose monoidratada. Estudou-se a influência do transportador e dos excessos de fármaco em relação ao rotulado no desempenho do DPI. Inaladores de dose calibrada (MDI) com propelentes à base de hidrofluoralcanos (HFA) foram formulados com várias doses, excessos de fármaco em relação ao rotulado e diferentes concentrações de álcool. Avaliaram-se as DPI e MDI formuladas por vários métodos oficiais e não oficiais de controle de qualidade. Estudaram-se a influência da superdosagem na liberação da válvula, o efeito dos excessos na dose emitida e a influência do álcool no padrão do spray do MDI. Obtiveram-se a melhor partícula fina e a dose emitida do DPI formulado com proporção de 10:90 de lactose fina:lactose grossa e 20% p/p de excesso. Os estudos em MDI revelaram que 15% de sobredose são requeridos para a liberação efetiva da válvula e 20% de excessos, para a liberação de 100% dos fármacos. Álcool a 5-10% v/v permitiu alcançar ótima dose emitida e fração de partícula fina.

Oral Beclomethasone Dipropionate for the Treatment of Steroid-refractory Gastrointestinal Acute Graft-versus-host Disease

Acute graft-versus-host disease (GVHD) is one of the most severe complications following allogeneic stem cell transplantation (SCT), and involvement of the gut has been associated with increased mortality and a poorer response to high-dose systemic corticosteroids. For over a decade, oral beclomethasone dipropionate (BDP) has been studied in the treatment of acute gastrointestinal GVHD, as a monotherapy, or in combination with systemic corticosteroids. Here we report, for the first time in Korea, the efficacy of oral BDP (8 mg/day for 25 days) in 3 adults with acute lymphoblastic leukemia who developed steroid-refractory gastrointestinal GVHD (grade III) after myeloablative conditioning SCT (1 matched sibling transplant, 2 matched unrelated transplants). All patients responded completely to oral BDP treatment. Oral BDP is safe and effective for the control of steroid-refractory acute gastrointestinal GVHD.

Fluticasone Propionate and Beclomethasone Dipropionate in Asthmatic Patients / 결핵

BACKGROUND: Corticosteroid is most potent and effective anti-inflammatory medication currently available and inhaled form has been used in the long-term control of asthma. Fluticasone propionate(Flixotide/Flovent : FP) is highly potent and topically active inhaled corticosteroid and has at least twice the potency of beclomethasone dipropionate(BDP) in the control of asthma. The aim of this study was to compare the efficacy of FP and BDP in several aspects. METHOD: Fifty patients with asthma were treated in a randomized, parallel group study of 4 weeks duration. During 2-week run-in period beta2-agonist was administered. After run-in period, FP 500 micro gram/day was administered via Diskhaler or BDP 800 micro gram/day via reservoir dry-power device. During the run-in and treatment period, morning and evening peak expiratory flow rate(PEFR) were measured daily. Daytime and night-time asthma symptoms, daytime and night-time rescue bronchodilator use were checked daily. FEV1.0 and FVC were measured biweekly in both groups. RESULTS: Three patients treated with FP and seven patient treated with BDP were dropped out. Therefore forty patients completed the study. Morning and evening PEFR was increased and diurnal variation of PEFR decreased significantly in both groups. FEV1.0 increased significantly in FP treatment group but not in BDP group. There were also improvements in daytime and night-time asthma symptoms, daytime and night-time rescue bronchodilator use in both groups after treatment. there were no significant difference between groups in any of the efficacy parameters. Therapeutic effects were dimonstrated earlier in patient treated with FP than BDP. CONCLUSION: In this study, 500 micro gram/day fluticasone propionate was as effective as 800 micro gram/day beclomethasone dipropionate in the control of asthma. Therapeutic effects were demonstrated earlier in patient treated with FP than BDP without adverse effect.

Effect of Inhaled Steroids on the Cortisol Concentration by Different Dosage or Delivery Method / 결핵

BACKGROUND: Topical inhaled steroids, budesonide(Bu) and beclomethasone dipropionate (BDP), are now established as effective drugs in the management of chronic asthma. These drugs have high topical anti-inflammatory effect with low systemic activity. This study was performed to determine the effects of two inhaled corticosteroids, Bu and BDP, on the adrenocortical supression in 44 patients with bronchial asthma or chronic obstructive pulmonary disease. METHODS: The adrenocortical function was assessed by measurement of serum cortisol concentration at 8 o'clock in morning and free cortisol in 24-hour urine collection at interval in 44 patients. No steroid was administered during the pretreatment period of 10 days and the final 6 days of the study. Each subject inhaled BDP or Bu, in daily doses of 800 or 1,600 micrograms for 12 days. The dose was delivered by metered dose inhaler (MDI) or diskhaler or large spacing device attached to MDI. RESULTS: The levels of serum cortisol and 24-hour urinary free cortisol were decreased during the treatment period in patients inhaled Bu delivered by MDI in daily doses of 800 and 1,600 micrograms. In contrast, serum cortisol level was decreased on 6 and 12th day of treatment period in patients with BDP diskhaler in daily doses of 800 micrograms. In daily doses of 1,600 micrograms, the serum cortisol and 24hour urine free cortisol levels were decreased on 6, 9 and 12th day of treatment period in patients with BDP disk haler. The serum cortisol and 24-hour urinary free cortisol levels were not significantly decreased during the treatment period in patients inhaled Bu delivered by large spacing device attached to a MDI. CONCLUSION: These results showed that 1) the endogenous cortisol secretion was suppressed after inhalation of BDP and Bu in daily doses of 800 and l,600micrograms, 2) Bu with MDI suppressed the adrenocortical function more than BDP with diskhaler, in daily doses of 1600 micrograms, and 3)large spacing device attached to a MDI might decrease the risk of suppression in the hypothalamic -pituitary- adrenal axis.