• Title/Summary/Keyword: topical drug

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Chronic postsurgical pain: current evidence for prevention and management

  • Thapa, Parineeta;Euasobhon, Pramote
    • The Korean Journal of Pain
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    • v.31 no.3
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    • pp.155-173
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    • 2018
  • Chronic postsurgical pain (CPSP) is an unwanted adverse event in any operation. It leads to functional limitations and psychological trauma for patients, and leaves the operative team with feelings of failure and humiliation. Therefore, it is crucial that preventive strategies for CPSP are considered in high-risk operations. Various techniques have been implemented to reduce the risk with variable success. Identifying the risk factors for each patient and applying a timely preventive strategy may help patients avoid the distress of chronic pain. The preventive strategies include modification of the surgical technique, good pain control throughout the perioperative period, and preoperative psychological intervention focusing on the psychosocial and cognitive risk factors. Appropriate management of CPSP patients is also necessary to reduce their suffering. CPSP usually has a neuropathic pain component; therefore, the current recommendations are based on data on chronic neuropathic pain. Hence, voltage-dependent calcium channel antagonists, antidepressants, topical lidocaine and topical capsaicin are the main pharmacological treatments. Paracetamol, NSAIDs and weak opioids can be used according to symptom severity, but strong opioids should be used with great caution and are not recommended. Other drugs that may be helpful are ketamine, clonidine, and intravenous lidocaine infusion. For patients with failed pharmacological treatment, consideration should be given to pain interventions; examples include transcutaneous electrical nerve stimulation, botulinum toxin injections, pulsed radiofrequency, nerve blocks, nerve ablation, neuromodulation and surgical management. Physical therapy, cognitive behavioral therapy and lifestyle modifications are also useful for relieving the pain and distress experienced by CPSP patients.

Study on the Influence of Cubic Liquid Crystalline Phases of Monoolein on the Stability and Transdermal Delivery of Retinylpalmitate (Monoolein액정상이 Retinylpalmitate의 안정성과 경피전달에 미치는 효과에 관한 연구)

  • Lee, Kyoung-Gum;Kang, Myung-Joo;Choi, Young-Wook;Lee, Jae-Hwi
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.243-247
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    • 2007
  • Retinoids have many important and diverse functions and particularly, have been widely used as anti-aging agent and for the treatment of acne and psoriasis in cosmetics. However, retinoids have low stability against the air, light, water, oxygen and heat, thus, to stabilize the retinoids in formulations is very critical procedure. In this study, cubic liquid crystalline phase of monoolein was applied to stabilize the retinylpalmitate (RP) and to enhance the transdermal permeation. Cubic liquid crystalline phase significantly enhanced the stability of RP. After 15 days, the content of RP in the cubic formulation was 94.7% while the content of RP in ethanol solution was below 0.5% at room temperature. Although BHT containing crystalline phase showed the slightly increased stability of RP, there were no significant differences in RP stability between with or without antioxidants (ascorbic acid, ${\alpha}$-tocopherol, BHT, BHA) at $40^{\circ}C$. The skin retention of RP in crystalline formulations was approximately $5.3{\sim}6.4$ times greater than that of o/w cream formulation. Incorporation of RP into cubic liquid crystalline phase of monoolein effectively stabilized the RP and worked as excellent topical vehicle for RP. Liquid crystalline phase is considered to be suitable formulation for RP for topical delivery system as a stabilizer and permeation enhancing agent.

Recombinant Human Epidermal Growth Factor (rhEGF)-loaded Solid Lipid Nanoparticles: Fabrication and Their Skin Accumulation Properties for Topical rhEGF Delivery

  • Hwang, Hee-Jin;Han, Sunhui;Jeon, Sangok;Seo, Joeun;Oh, Dongho;Cho, Seong-Wan;Choi, Young Wook;Lee, Sangkil
    • Bulletin of the Korean Chemical Society
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    • v.35 no.8
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    • pp.2290-2294
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    • 2014
  • For the present study, rhEGF was encapsulated into solid lipid nanoparticles (SLNs). The SLNs were prepared by the $W_1/O/W_2$ double emulsification method combined with the high pressure homogenization method and the physical properties such as particle size, zeta-potential and encapsulation efficiency were measured. The overall particle morphology of SLNs was investigated using a transmission electron microscopy (TEM). The percutaneous skin permeation and accumulation property of rhEGF was evaluated using Franz diffusion cell system along with confocal laser scanning microscopy (CLSM). The mean particle size of rhEGF-loaded SLNs was $104.00{\pm}3.99nm$ and the zeta-potential value was in the range of -$36.99{\pm}0.54mV$, providing a good colloidal stability. The TEM image revealed a spherical shape of SLNs about 100 nm and the encapsulation efficiency was $18.47{\pm}0.22%$. The skin accumulation of rhEGF was enhanced by SLNs. CLSM image analysis provided that the rhEGF rat skin accumulation is facilitated by an entry of SLNs through the pores of skin.

Persicaria senticosa Ameliorates Imiquimod-induced Psoriasis-like Skin Lesions in Mice via Suppression of IL-6/STAT3 Expression and Proliferation of Keratinocytes

  • Jung, Sangmi;Park, Jeong-Ran;Ra, Moonjin;Kim, Young Han;Yu, Ji Hoon;Lee, Yongjun
    • Natural Product Sciences
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    • v.26 no.2
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    • pp.136-143
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    • 2020
  • Psoriasis is one of the most common inflammatory skin disorders, with a global prevalence of 2% - 3%. It is an autoimmune skin disorder characterized by excessive generation of plaques on the skin with typical long-lasting red, itchy, and scaly lesions. In this study, we aimed to elucidate the anti-psoriatic effect of the methanolic extract of Persicaria senticosa (PS), a bioactive edible plant extract used in traditional medicine, using a mouse model of imiquimod (IMQ)-induced psoriasis. The daily topical application of IMQ could induce human psoriasis-like lesion. The extract ameliorated IMQ-induced psoriasis. Furthermore, hematoxylin and eosin staining and the Psoriasis Area and Severity Index (PASI) scores indicated that topical application of PS led to an improvement in erythema, scaling, and thickness scores of the mouse dorsal skin and a considerable decrease in the epidermal thickness of the ear and dorsal skin in the IMQ-induced psoriatic mouse model. We also studied the effect of PS on the proliferation of keratinocytes using HaCaT cells. The extract inhibited cell proliferation and IL-6 and pSTAT3 expression induced by M5 cocktail (comprising interleukin [IL]-1α, IL-17A, IL-22, oncostatin M, and tumor necrosis factor-α) in HaCaT cells. Thus, PS might serve as a potential therapeutic agent for the treatment of psoriasis.

Screening of Antioxidative Effect and Suppressive Effect of LDL Oxidation of Euryale ferox Salisbury (Euryale ferox Salisbury의 항산화효과 및 LDL 산화 억제효과 탐색)

  • Kim, Young-Hwan;Lee, Min-Ja;Lee, Hye-Sook;Kim, Jung-Guk;Park, Won-Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.25 no.1
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    • pp.92-99
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    • 2011
  • Topical natural antioxidants are a useful strategy for the prevention of oxidative stress mediated cardiovascular disease including atherosclerosis. From the viewpoint of this underlying principle, the screening of natural plant extracts with scavenging activity for pro-oxidant reactive species is a primary requirement for the development of new topical antioxidant formulations. Euryale ferox Salisbury (EF) is botanical name and it's pharmaceutical name is EURYALES SEMEN (ES). The stems and branchs of EF have been used as a traditional herbal medicine for the treatment of dysentery, diarrhea, leucorrhoea, incontinence and paralysis of joint. In this study, the antioxidant activity of extract from EF was studied in vitro methods by measuring the antioxidant activity and free radical scavenging activity by TEAC and DPPH, measuring the scavenging effects on reactive oxygen species (ROS) [superoxide anion, hydroxyl radical] and on reactive nitrogen species (RNS) [nitric oxide and peroxynitrite] as well as measuring the inhibitory effect on $Cu^{2+}$-induced human LDL oxidation. The EF extracts were found to have a potent scavenging activity, as well as an inhibitory effect on LDL oxidation. In conclusion, the EF extracts have antioxidative effects in vitro system, which can be used for developing pharmaceutical drug against oxidative stress and chronic degenerative disease such as atherosclerosis.

A Randomized Active Controlled Clinical Trial to Evaluate Safety and Efficacy of a Topical Unani Formulation Marham Kharish Jadeed in the Management of Qūbā (Tinea Corporis)

  • Aaliya, Aaliya;Nawab, Mohammad;Kazmi, M.H.;Ayyub, Sana
    • CELLMED
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    • v.10 no.3
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    • pp.22.1-22.7
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    • 2020
  • Introduction: Qūbā (Tinea Corporis) is a very common disease widely prevalent worldwide. 20 - 25 % individuals suffer for this stubborn disease. Unani System of Medicine offers its treatment. There are many pharmacopoeial formulations indicated for various types of dermatophytic infections. In this study clinical efficacy and safety of the topical Unani formulation Marham Kharish Jadeed (a compound drug in the dosage form of an ointment) was assessed and compared with a standard conventional medicine. Materials and methods: A clinical study was conducted on 60 participants of qūbā randomized into test and control groups (n=30 in each group). The participants were clinically diagnosed and confirmed by microscopy of skin scrapings. The efficacy of the Unani formulation was assessed in terms of TSS score and elimination of fungal elements from the skin lesions. The data collected were analyzed statistically. Results and discussion: The study showed that the Unani formulation had comparatively better efficacy clinically than conventional medicine Terbinafine hydrochloride 1% cream in terms of reduction of itching, erythema, scaling, peripheral raised margins of the lesion comparing to baseline. In this study, 27 participants in test group and 18 participants in control group were completely cured (≥75% reduction in TSS Score with Mycological Cure) after 4 weeks of treatment. The efficacy of the Unani formulation was found significant statistically. The individual drugs of the formulations having analgesic (Musakkin), blood purifier (Muṣaffi-i-Dam), demulcent (Mulaṭṭif), antifungal (Qātil-i-fafūndῑ), detergent (Jālῑ), refrigerant (Mubarrid) and antiseptic (Dāfi'-i-'Ufūnat) properties might be responsible for the efficacy of Unani formulation. Conclusion: The findings of the study suggested that the Unani formulation was found effective and safe in the management of qūbā. No local and systemic adverse effect was reported during the study.

Repurposing Auranofin, an Anti-Rheumatic Gold Compound, to Treat Acne Vulgaris by Targeting the NLRP3 Inflammasome

  • Yang, Gabsik;Lee, Seon Joo;Kang, Han Chang;Cho, Yong-Yeon;Lee, Hye Suk;Zouboulis, Christos C.;Han, Sin-Hee;Ma, Kyung-Ho;Jang, Jae-Ki;Lee, Joo Young
    • Biomolecules & Therapeutics
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    • v.28 no.5
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    • pp.437-442
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    • 2020
  • Activation of the NLRP3 inflammasome is critical for host defense as well as the progression of inflammatory diseases through the production of the proinflammatory cytokine IL-1β, which is cleaved by active caspase-1. It has been reported that overactivation of the NLRP3 inflammasome contributes to the development and pathology of acne vulgaris. Therefore, inhibiting activation of the NLRP3 inflammasome may provide a new therapeutic strategy for acne vulgaris. In this study, we investigated whether auranofin, an anti-rheumatoid arthritis agent, inhibited NLRP3 inflammasome activation, thereby effectively treating acne vulgaris. Auranofin suppressed NLRP3 inflammasome activation induced by Propionibacterium acnes, reducing the production of IL-1β in primary mouse macrophages and human sebocytes. In a P. acnes-induced acne mouse model, injection of P. acnes into the ears of mice induced acne symptoms such as redness, swelling, and neutrophil infiltration. Topical application of auranofin (0.5 or 1%) to mouse ears significantly reduced the inflammatory symptoms of acne vulgaris induced by P. acnes injection. Topical application of auranofin led to the downregulation of the NLRP3 inflammasome activated by P. acnes in mouse ear skin. These results show that auranofin inhibits the NLRP3 inflammasome, the activation of which is associated with acne symptoms. The results further suggest that topical application of auranofin could be a new therapeutic strategy for treating acne vulgaris by targeting the NLRP3 inflammasome.

Effect of electro-acupuncture ST36 on altered transmission of afferent somatosensory information caused by amyloid-β (전침(電鍼)이 amyloid-β에 의한 구심성 체감각 신경정보전달 변화에 미치는 영향)

  • Lee, Hyun-jong;Kim, Chang-hwan;Lee, Yun-ho
    • Journal of Acupuncture Research
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    • v.20 no.4
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    • pp.145-156
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    • 2003
  • Objective : This study is to investigate the effect of electro-acupuncture ST36 on altered transmission of afferent somatosensory information caused by amyloid-${\beta}$(A-${\beta}$) that caused Alzheimer's disease. Methods : The effects of topical application of A-${\beta}$, A-${\beta}$ with ST36, aggregated A-${\beta}$(aA-${\beta}$), aA-${\beta}$ with ST36 and ST36 on the afferent sensory transmission to the neurons in the primary somatosensory(SI) cortex was observed in anesthetized rats. Quantitative determination of the effects of A-${\beta}$, A-${\beta}$ with ST36, aA-${\beta}$, aA-${\beta}$ with ST36 and ST36 was made by generating poststimulus time histogram of evoked response of individual cortical neuron by electrical stimulation of the receptive located in peripheral area(forepaw) Results : The results obtained in present study were summerized as follow : 1. Application of physiological concentrative 0.5 nM A-${\beta}$ caused afferent sensory transmission of SI cortex facilitated. 0.5 nM A-${\beta}$ with ST36 exerted much stronger effects than 0.5 nM A-${\beta}$ alone. 2. Application of $10{\mu}M$ A-${\beta}$ caused afferent sensory transmission of SI cortex unchangeable. But $10{\mu}M$ A-${\beta}$ with ST36 is facilitated at 30 min of post-drug period 3. Application of $10{\mu}M$ aA-${\beta}$ caused afferent sensory transmission of SI cortex diminished. $10{\mu}M$ aA-${\beta}$ with ST36 is diminished after 15min of post-drug period but is facilitated after 75min.

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Effect of Charge Carrier Lipid on Skin Penetration, Retention, and Hair Growth of Topically Applied Finasteride-Containing Liposomes

  • Lee, Sang-Im;Nagayya-Sriraman, Santhosh-Kumar;Shanmugam, Srinivasan;Baskaran, Rengarajan;Yong, Chul-Soon;Yoon, Sang-Kwon;Choi, Han-Gon;Yoo, Bong-Kyu
    • Biomolecules & Therapeutics
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    • v.19 no.2
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    • pp.231-236
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    • 2011
  • The aim of this study was to investigate the effect of charge carrier lipid on the skin penetration, retention, and hair growth of topically applied finasteride-containing liposomes. Finasteride-containing liposomes were prepared by traditional thin film hydration method using Phospholipon$^{(R)}$ 85 G and cholesterol with or without charge carrier lipid (1,2 dimyristoyl-sn-glycero-3-phosphate or 1,2-dioleoyl-trimethylammonium-propane for anionic and cationic charge, respectively). Freshly prepared finasteride-containing liposome suspension was applied on the hairless mouse skin, and skin penetration and retention were measured using Keshary-Chien diffusion cell. Non-liposomal formulation (ethanol 10% solution containing 0.5 mg/ml of FNS) was also used as a control. The amount of finasteride in the diffusion cell and mouse skin was measured by HPLC. The hair growth was evaluated using depilated male C57BL/6N mice. Mean particle size of all finasteride-containing liposomes was less than a micron, and polydispersity index revealed size homogeneity. Skin penetration and retention studies showed that significantly less amount of finasteride was penetrated when applied as anionic liposome while more amount of the drug was retained. Specifically, in liposome prepared with 10% anionic charge carrier lipid, penetration was 12.99 ${\mu}g/cm^2$ while retention was 79.23 ${\mu}g/cm^2$ after 24 h of application. In hair growth study, finasteride-containing anionic liposomes showed moderate efficacy, but the efficacy was not found when applied as cationic liposomes. In conclusion, topical application of finasteride using anionic liposome formulation appears to be useful option for the treatment of androgenetic alopecia to avoid systemic side effects of the drug.

Retrospective Review of Effectiveness of Various Pharmacological Agents in Treating Burning Mouth Syndrome

  • Im, Yeong-Gwan;Kim, Byung-Gook;Kim, Jae-Hyung
    • Journal of Oral Medicine and Pain
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    • v.41 no.1
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    • pp.21-25
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    • 2016
  • Purpose: Burning mouth syndrome (BMS) is a chronic pain condition involving the oral and perioral regions, often characterized by a burning sensation and pain in elderly patients. In this study, we investigated the effectiveness of pharmacological agents for the treatment of BMS patients through a retrospective chart review. Methods: We enrolled 61 BMS subjects (57 females, 4 males; $66.4{\pm}10.9$ years of age) from among consecutive patients treated pharmacologically from January 2014 to June 2015 at Chonnam National University Dental Hospital. Patients with secondary BMS associated with local factors were excluded. The treatment period, number of pharmacological agents tried, and effectiveness of the drugs administered to each subject were analyzed. Results: The mean treatment period for the management of BMS was 2.5 months. More than three agents were tried to control BMS symptoms in 17 subjects (27.9%); two agents were used in 10 subjects (16.4%), and a single agent in 24 subjects (39.3%). Clonazepam was prescribed most frequently and was effective at relieving symptoms in 30 of 39 subjects (76.9%). Paroxetine was moderately effective, relieving symptoms in 7 of 17 subjects (41.2%). Some of the subjects benefited from tricyclic antidepressants, gabapentin, and lipoic acid. A topical local anesthetic used to supplement other systemic agents had ameliorating effects in four of six subjects. Conclusions: Within the study limitations, clonazepam was the most effective drug and antidepressants were efficacious in some subjects for relieving the symptoms of BMS. These pharmacological agents could be considered as first-line drugs for the management of BMS.