A betamethasone dipropionate (BD) liposomal cream was developed to treat rheumatological, inflammatory, allergic diseases and psoriasis. BD is a corticosteroid, anti-inflammatory, and immunosuppressant. However, adver...A betamethasone dipropionate (BD) liposomal cream was developed to treat rheumatological, inflammatory, allergic diseases and psoriasis. BD is a corticosteroid, anti-inflammatory, and immunosuppressant. However, adverse effects are associated with prolonged topical use. For this reason, liposomes were loaded with BD because they offer excellent biocompatibility, bio adhesiveness, and penetrability that improve the effects caused by the conventional drug. Liposomal dispersions were prepared by emulsification using phospholipid 90 (lipid) and Tween 80 (surfactant). The particle size, polydispersity index (PDI), and zeta potential were measured using a particle analyzer. The betamethasone (BM) percentage of encapsulated active (EA) ingredient was also determined through High Performance Liquid Chromatography (HPLC). The Franz cell and tape stripping characterized these in vitro and ex vivo. Then the final formulation reached a particle size of 70.80 ± 3.31 nm, a PDI of 0.242 ± 0.038, a zeta potential of −11.68 ± 0.77 mv and encapsulate active of 83.1% ± 2.4, complying with the parameters of a nanotechnological formulation. In vitro and ex vivo studies confirmed significantly efficacy of the cream over the commercial product, through the greater penetration into the pig ear skin, resulting in an improved drug. Finally, the liposomal cream demonstrated significant potential for enhanced percutaneous absorption, attributed to its nanometric size. This innovative nanotechnology approach aims to reduce the frequency of topical applications, thereby minimizing the side effects associated with psoriasis treatment.展开更多
Scar hyperplasia at the suture site is an important reason for hindering the repair effect of peripheral nerve injury anastomosis. To address this issue, two repair methods are often used. Biological agents are used t...Scar hyperplasia at the suture site is an important reason for hindering the repair effect of peripheral nerve injury anastomosis. To address this issue, two repair methods are often used. Biological agents are used to block nerve sutures and the surrounding tissue to achieve phys- ical anti-adhesion effects. Another agent is glucocorticosteroid, which can prevent scar growth by inhibiting inflammation. However, the overall effect of promoting regeneration of the injured nerve is not satisfactory. In this regard, we envision that these two methods can be combined and lead to shared understanding for achieving improved nerve repair. In this study, the right tibial nerve was transected 1 cm above the knee to establish a rat tibial nerve injury model. The incision was directly sutured after nerve transection. The anastomotic stoma was coated with 0.5 × 0.5 cm^2 chitosan sheets with betamethasone dipropionate. At 12 weeks after injury, compared with the con- trol and poly (D, L-lactic acid) groups, chitosan-betamethasone dipropionate film slowly degraded with the shape of the membrane still intact. Further, scar hyperplasia and the degree of adhesion at anastomotic stoma were obviously reduced, while the regenerated nerve fiber structure was complete and arranged in a good order in model rats. Electrophysiological study showed enhanced compound muscle action potential. Our results confirm that chitosan-betamethasone dipropionate film can effectively prevent local scar hyperplasia after tibial nerve repair and promote nerve regeneration.展开更多
The purpose of this study was to design an innovative topical ointment containing betamethasone dipropionate loaded nanostructured lipid carrier (BD-NLC) for the treatment of atopic dermatitis (AD). BD-loaded NLC was ...The purpose of this study was to design an innovative topical ointment containing betamethasone dipropionate loaded nanostructured lipid carrier (BD-NLC) for the treatment of atopic dermatitis (AD). BD-loaded NLC was produced with precirol ATO 5 and oleic oil (OA) by melt emulsification method. Effects of surfactant concentration, amount of solid lipid and liquid lipid on skin retention and skin penetration were investigated by in vitro percutaneous permeation experiment. The optimized BD-NLC showed a homogeneous particle size of 169.1 nm (with PI = 0.195), negatively charged surface (-23.4 mV) and high encapsulation efficiency (85%). Particle morphology assessed by TEM revealed a spherical shape. In vitro skin permeation study was carried out to investigate the percutaneous behaviors of W/O ointment with BD-NLC and Carbopol emulgel ointment with BD-NLC. W/O ointment with BDNLC showed high skin retention (35.43 μg/g) and low penetration (0.87 μg/ml). In vitro drug release studies were carried out to demonstrate the drug releasing properties of the two ointments. W/O ointment with BD-NLC showed an advantage for skin retention as it was better for drug release. The tissue distribution test suggested that BD distribution was skin > muscle > blood. Self-made topical ointment in mice showed no skin irritation. The animal experiments indicated that BD-loaded NLC ointment was effective and safe for topical use.展开更多
Objective:To investigate the efficacy and safety of intra-articular injection of low-dose compound betamethasone in the treatment of mild knee osteoarthritis.Methods:From September 2018 to December 2019,90 patients wi...Objective:To investigate the efficacy and safety of intra-articular injection of low-dose compound betamethasone in the treatment of mild knee osteoarthritis.Methods:From September 2018 to December 2019,90 patients with mild knee osteoarthritis were divided into complete dose group and low dose group according to the treatment sequence,45 cases in each group.The complete dose group was treated with intra-artiular injection of betamethasone(1ml)and sodium hyaluronate(2ml),once a week,three times as a course of treatment.The low dose group was treated with intra-artiular injection of betamethasone(0.3ml)and sodium hyaluronate(2ml),once a week,three times as a course of treatment.Lysholm scores、the Western Ontario and McMaster Universities Osteoarthritis Index(WOMAC)and visual analogue scale(VAS)were compared between the two groups before and after treatment,and the efficacy and safety of the two groups were evaluated.Results:80 patients were followed up with an average of(4.96±1.50)months ranging from 3 to 8 months,and 10 cases(11.11%)were dropped out,including 2 cases in the complete dose group,2 cases in the midway withdrawal group,and 1 case in the treatment course less than the treatment course;3 cases in the low dose group lost the follow-up,and 2 cases dropped out.Compared with that before treatment,Lysholm scores were significantly improved,WOMAC scores and VAS scores were significantly decreased in the two groups at 3 weeks,6 weeks and 12 weeks after treatment(P<0.001).The Lysholm scores of low dose group were78.10±2.16,86.78±2.55,80.90±2.26,WOMAC scores were 61.00±1.38,39.03±1.98,45.76±1.66 and VAS scores were 2.23±0.89,0.78±0.73 and 1.05±0.85 in low dose group at 3 weeks,6 weeks and 12 weeks after treatment.There was no significant difference between the two groups(P>0.05).No drugrelated adverse reactions occurred in both groups.Conclusion:The curative effect of low dose compound betamethasone intra-articular injection in the treatment of mild knee osteoarthritis is equivalent to that of complete dose compound betamethasone.It can improve the function and symptoms of knee joint,and is safe and effective.展开更多
<strong>Objective: </strong><span style="font-family:Verdana;">To assess whether the use of prenatal betamethasone in pregnancies with elective Caesarean section (C-section) at 38 weeks ha&...<strong>Objective: </strong><span style="font-family:Verdana;">To assess whether the use of prenatal betamethasone in pregnancies with elective Caesarean section (C-section) at 38 weeks ha</span><span style="font-family:Verdana;">s</span><span style="font-family:""><span style="font-family:Verdana;"> a similar risk of adverse neonatal respiratory outcomes than elective C-section at 39 weeks. </span><b><span style="font-family:Verdana;">Methods:</span></b><span style="font-family:Verdana;"> Retrospective cohort study of pregnant patients with singleton pregnancies and elective C-section at term in a one-year period. Cases were C-section at 38 weeks of gestation with a complete course of betamethasone started 48-hours before. As a control group, pregnancies with a C-section at 39 weeks without betamethasone were included. </span><b><span style="font-family:Verdana;">Results:</span></b><span style="font-family:Verdana;"> During the study period, 186 patients were included. Of these, 91 were delivered at 38 weeks and 95 at 39 weeks. There were no significant differences in maternal age and parity. Moreover, there were no significant differences in respiratory complications (respiratory distress syndrome [RDS] = 0% vs 1.1%;p</span></span><span style="font-family:""> </span><span style="font-family:Verdana;">=</span><span style="font-family:""> </span><span style="font-family:Verdana;">1.0, transitory tachypnea [TT] = 0% vs 0%) and admission to Neonatal Intensive Care Unit (NICU) (8.8% vs 6.3%;p</span><span style="font-family:""> </span><span style="font-family:Verdana;">=</span><span style="font-family:""> </span><span style="font-family:""><span style="font-family:Verdana;">0.7) between deliveries at 38 weeks and 39 weeks, respectively. </span><b><span style="font-family:Verdana;">Conclusion:</span></b><span style="font-family:Verdana;"> Prophylactic use of betamethasone in early term pregnancies who undergo an elective C-section at 38 weeks is associated with similar adverse neonatal respiratory outcomes than patients with C-section at 39 weeks without corticosteroids.</span></span>展开更多
Introduction:Acrodermatitis continua of Hallopeau(ACH)is an uncommon chronic cutaneous disorder.Up to date,its treatment is still difficult and frustrating although various topical and systemic agents alone or in diff...Introduction:Acrodermatitis continua of Hallopeau(ACH)is an uncommon chronic cutaneous disorder.Up to date,its treatment is still difficult and frustrating although various topical and systemic agents alone or in different combinations have been tried with variable benefits.Herein,we report two cases of ACH successfully treated with calcipotriol/betamethasone ointment.Case presentation:Two cases of ACH were characterized by thumb involvement alone and showed an excellent response to calcipotriol/betamethasone ointment(1 g:calcipotriol 50µg and betamethasone 0.5 mg).Discussion:Treatment of ACH is challenging for physicians.Multiple systemic therapies and topical drugs have been applied,however,no universally effective treatment regimen has yet been established for long-lasting remission.Combination of calcipotriol and betamethasone is more effective in treating psoriasis than the individual components alone,and the current 2 cases with ACH were reported to be treated successfully by the calcipotriol/betamethasone ointment.Conclusion:Topical calcipotriol/betamethasone compound is an optional agent for the treatment of ACH with a novel effect.展开更多
A formal synthesis of betamethasone from 5α-pregnane-3β,16β,20S-triol is described.Key transformations are a bromination-acetylation of triol,an SN2 reaction of the resulting C16α-bromide with dimethylcopperlithiu...A formal synthesis of betamethasone from 5α-pregnane-3β,16β,20S-triol is described.Key transformations are a bromination-acetylation of triol,an SN2 reaction of the resulting C16α-bromide with dimethylcopperlithium to get the required C16β-methyl group,and a double hydroxylation to prepare the dihydroxyacetone side chain.展开更多
文摘A betamethasone dipropionate (BD) liposomal cream was developed to treat rheumatological, inflammatory, allergic diseases and psoriasis. BD is a corticosteroid, anti-inflammatory, and immunosuppressant. However, adverse effects are associated with prolonged topical use. For this reason, liposomes were loaded with BD because they offer excellent biocompatibility, bio adhesiveness, and penetrability that improve the effects caused by the conventional drug. Liposomal dispersions were prepared by emulsification using phospholipid 90 (lipid) and Tween 80 (surfactant). The particle size, polydispersity index (PDI), and zeta potential were measured using a particle analyzer. The betamethasone (BM) percentage of encapsulated active (EA) ingredient was also determined through High Performance Liquid Chromatography (HPLC). The Franz cell and tape stripping characterized these in vitro and ex vivo. Then the final formulation reached a particle size of 70.80 ± 3.31 nm, a PDI of 0.242 ± 0.038, a zeta potential of −11.68 ± 0.77 mv and encapsulate active of 83.1% ± 2.4, complying with the parameters of a nanotechnological formulation. In vitro and ex vivo studies confirmed significantly efficacy of the cream over the commercial product, through the greater penetration into the pig ear skin, resulting in an improved drug. Finally, the liposomal cream demonstrated significant potential for enhanced percutaneous absorption, attributed to its nanometric size. This innovative nanotechnology approach aims to reduce the frequency of topical applications, thereby minimizing the side effects associated with psoriasis treatment.
文摘Scar hyperplasia at the suture site is an important reason for hindering the repair effect of peripheral nerve injury anastomosis. To address this issue, two repair methods are often used. Biological agents are used to block nerve sutures and the surrounding tissue to achieve phys- ical anti-adhesion effects. Another agent is glucocorticosteroid, which can prevent scar growth by inhibiting inflammation. However, the overall effect of promoting regeneration of the injured nerve is not satisfactory. In this regard, we envision that these two methods can be combined and lead to shared understanding for achieving improved nerve repair. In this study, the right tibial nerve was transected 1 cm above the knee to establish a rat tibial nerve injury model. The incision was directly sutured after nerve transection. The anastomotic stoma was coated with 0.5 × 0.5 cm^2 chitosan sheets with betamethasone dipropionate. At 12 weeks after injury, compared with the con- trol and poly (D, L-lactic acid) groups, chitosan-betamethasone dipropionate film slowly degraded with the shape of the membrane still intact. Further, scar hyperplasia and the degree of adhesion at anastomotic stoma were obviously reduced, while the regenerated nerve fiber structure was complete and arranged in a good order in model rats. Electrophysiological study showed enhanced compound muscle action potential. Our results confirm that chitosan-betamethasone dipropionate film can effectively prevent local scar hyperplasia after tibial nerve repair and promote nerve regeneration.
文摘The purpose of this study was to design an innovative topical ointment containing betamethasone dipropionate loaded nanostructured lipid carrier (BD-NLC) for the treatment of atopic dermatitis (AD). BD-loaded NLC was produced with precirol ATO 5 and oleic oil (OA) by melt emulsification method. Effects of surfactant concentration, amount of solid lipid and liquid lipid on skin retention and skin penetration were investigated by in vitro percutaneous permeation experiment. The optimized BD-NLC showed a homogeneous particle size of 169.1 nm (with PI = 0.195), negatively charged surface (-23.4 mV) and high encapsulation efficiency (85%). Particle morphology assessed by TEM revealed a spherical shape. In vitro skin permeation study was carried out to investigate the percutaneous behaviors of W/O ointment with BD-NLC and Carbopol emulgel ointment with BD-NLC. W/O ointment with BDNLC showed high skin retention (35.43 μg/g) and low penetration (0.87 μg/ml). In vitro drug release studies were carried out to demonstrate the drug releasing properties of the two ointments. W/O ointment with BD-NLC showed an advantage for skin retention as it was better for drug release. The tissue distribution test suggested that BD distribution was skin > muscle > blood. Self-made topical ointment in mice showed no skin irritation. The animal experiments indicated that BD-loaded NLC ointment was effective and safe for topical use.
基金General project of national natural science foundation of China(No.81473695)2019 Clinical collaborative capacity building project of traditional Chinese and western medicine for major and difficult diseases(No.201803190106)。
文摘Objective:To investigate the efficacy and safety of intra-articular injection of low-dose compound betamethasone in the treatment of mild knee osteoarthritis.Methods:From September 2018 to December 2019,90 patients with mild knee osteoarthritis were divided into complete dose group and low dose group according to the treatment sequence,45 cases in each group.The complete dose group was treated with intra-artiular injection of betamethasone(1ml)and sodium hyaluronate(2ml),once a week,three times as a course of treatment.The low dose group was treated with intra-artiular injection of betamethasone(0.3ml)and sodium hyaluronate(2ml),once a week,three times as a course of treatment.Lysholm scores、the Western Ontario and McMaster Universities Osteoarthritis Index(WOMAC)and visual analogue scale(VAS)were compared between the two groups before and after treatment,and the efficacy and safety of the two groups were evaluated.Results:80 patients were followed up with an average of(4.96±1.50)months ranging from 3 to 8 months,and 10 cases(11.11%)were dropped out,including 2 cases in the complete dose group,2 cases in the midway withdrawal group,and 1 case in the treatment course less than the treatment course;3 cases in the low dose group lost the follow-up,and 2 cases dropped out.Compared with that before treatment,Lysholm scores were significantly improved,WOMAC scores and VAS scores were significantly decreased in the two groups at 3 weeks,6 weeks and 12 weeks after treatment(P<0.001).The Lysholm scores of low dose group were78.10±2.16,86.78±2.55,80.90±2.26,WOMAC scores were 61.00±1.38,39.03±1.98,45.76±1.66 and VAS scores were 2.23±0.89,0.78±0.73 and 1.05±0.85 in low dose group at 3 weeks,6 weeks and 12 weeks after treatment.There was no significant difference between the two groups(P>0.05).No drugrelated adverse reactions occurred in both groups.Conclusion:The curative effect of low dose compound betamethasone intra-articular injection in the treatment of mild knee osteoarthritis is equivalent to that of complete dose compound betamethasone.It can improve the function and symptoms of knee joint,and is safe and effective.
文摘<strong>Objective: </strong><span style="font-family:Verdana;">To assess whether the use of prenatal betamethasone in pregnancies with elective Caesarean section (C-section) at 38 weeks ha</span><span style="font-family:Verdana;">s</span><span style="font-family:""><span style="font-family:Verdana;"> a similar risk of adverse neonatal respiratory outcomes than elective C-section at 39 weeks. </span><b><span style="font-family:Verdana;">Methods:</span></b><span style="font-family:Verdana;"> Retrospective cohort study of pregnant patients with singleton pregnancies and elective C-section at term in a one-year period. Cases were C-section at 38 weeks of gestation with a complete course of betamethasone started 48-hours before. As a control group, pregnancies with a C-section at 39 weeks without betamethasone were included. </span><b><span style="font-family:Verdana;">Results:</span></b><span style="font-family:Verdana;"> During the study period, 186 patients were included. Of these, 91 were delivered at 38 weeks and 95 at 39 weeks. There were no significant differences in maternal age and parity. Moreover, there were no significant differences in respiratory complications (respiratory distress syndrome [RDS] = 0% vs 1.1%;p</span></span><span style="font-family:""> </span><span style="font-family:Verdana;">=</span><span style="font-family:""> </span><span style="font-family:Verdana;">1.0, transitory tachypnea [TT] = 0% vs 0%) and admission to Neonatal Intensive Care Unit (NICU) (8.8% vs 6.3%;p</span><span style="font-family:""> </span><span style="font-family:Verdana;">=</span><span style="font-family:""> </span><span style="font-family:""><span style="font-family:Verdana;">0.7) between deliveries at 38 weeks and 39 weeks, respectively. </span><b><span style="font-family:Verdana;">Conclusion:</span></b><span style="font-family:Verdana;"> Prophylactic use of betamethasone in early term pregnancies who undergo an elective C-section at 38 weeks is associated with similar adverse neonatal respiratory outcomes than patients with C-section at 39 weeks without corticosteroids.</span></span>
文摘Introduction:Acrodermatitis continua of Hallopeau(ACH)is an uncommon chronic cutaneous disorder.Up to date,its treatment is still difficult and frustrating although various topical and systemic agents alone or in different combinations have been tried with variable benefits.Herein,we report two cases of ACH successfully treated with calcipotriol/betamethasone ointment.Case presentation:Two cases of ACH were characterized by thumb involvement alone and showed an excellent response to calcipotriol/betamethasone ointment(1 g:calcipotriol 50µg and betamethasone 0.5 mg).Discussion:Treatment of ACH is challenging for physicians.Multiple systemic therapies and topical drugs have been applied,however,no universally effective treatment regimen has yet been established for long-lasting remission.Combination of calcipotriol and betamethasone is more effective in treating psoriasis than the individual components alone,and the current 2 cases with ACH were reported to be treated successfully by the calcipotriol/betamethasone ointment.Conclusion:Topical calcipotriol/betamethasone compound is an optional agent for the treatment of ACH with a novel effect.
文摘A formal synthesis of betamethasone from 5α-pregnane-3β,16β,20S-triol is described.Key transformations are a bromination-acetylation of triol,an SN2 reaction of the resulting C16α-bromide with dimethylcopperlithium to get the required C16β-methyl group,and a double hydroxylation to prepare the dihydroxyacetone side chain.