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1.
Curr Top Med Chem ; 2024 Jan 29.
Artículo en Inglés | MEDLINE | ID: mdl-38288805

RESUMEN

BACKGROUND: The genus Costus is the largest genus in the family Costaceae and encompasses about 150 known species. Among these, Costus pictus D. Don (Synonym: Costus mexicanus) is a traditional medicinal herb used to treat diabetes and other ailments. Currently, available treatment options in modern medicine have several adverse effects. Herbal medicines are gaining importance as they are cost-effective and display improved therapeutic effects with fewer side effects. Scientists have been seeking therapeutic compounds in plants, and various in vitro and in vivo studies report Costus pictus D. Don as a potential source in treating various diseases. Phytochemicals with various pharmacological properties of Costus pictus D. Don, viz. anticancer, anti-oxidant, diuretic, analgesic, and anti-microbial have been worked out and reported in the literature. OBJECTIVE: The aim of the review is to categorize and summarize the available information on phytochemicals and pharmacological properties of Costus pictus D. Don and suggest outlooks for future research. METHODS: This review combined scientific data regarding the use of Costus pictus D. Don plant for the management of diabetes and other ailments. A systematic search was performed on Costus pictus plant with anti-diabetic, anti-cancer, anti-microbial, anti-oxidant, and other pharmacological properties using several search engines such as Google Scholar, PubMed, Science Direct, SciFinder, other online journals and books for detailed analysis. RESULTS: Research data compilation and critical review of the information would be beneficial for further exploration of its pharmacological and phytochemical aspects and, consequently, new drug development. Bioactivity-guided fractionation, isolation, and purification of new chemical entities from the plant as well as pharmacological evaluation of the same will lead to the search for safe and effective novel drugs for better healthcare. CONCLUSION: This review critically summarizes the reports on natural compounds, and different extract of Costus pictus D. Don with their potent anti-diabetic activity along with other pharmacological activity. Since this review has been presented in a very interactive manner showing the geographical region of availability, parts of plant used, mechanism of action and phytoconstituents in different extracts of Costus pictus responsible for particular action, it will be of great importance to the interested readers to focus on the development of the new drug leads for the treatment of diseases.

2.
Life Sci ; 328: 121909, 2023 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-37414141

RESUMEN

AIMS: Psoriasis is an immune-mediated skin disease characterized by keratinocytes hyperproliferation, abnormal differentiation and inflammation. Therefore, this study aimed to investigate in-vitro and in-vivo anti-inflammatory and anti-proliferative activity to evaluate anti-psoriatic potential of apigenin. MAIN METHODS: For in-vivo study, 5 % imiquimod cream was used to induce psoriasis-like skin inflammation in BALB/c mice to mimic human psoriatic conditions. PASI score, CosCam score, histopathology, immunohistochemistry, qRT-PCR, and ELISA were done to evaluate the anti-psoriatic potential of topically applied apigenin. For in-vitro studies, LPS-induced inflammation in RAW 264.7 was done, and qRT-PCR, ELISA, and immunofluorescence were conducted to evaluate the anti-inflammatory activity of apigenin. Migration and cell doubling assay in HaCaT cells were performed to assess the anti-proliferative effect of apigenin. Acute dermal toxicity profile of apigenin has also been done as per OECD guidelines. KEY FINDINGS: Results showed that apigenin significantly reduce the PASI and CosCam scores, ameliorate the deteriorating histopathology, and effectively downregulated the expression of CCR6, IL-17A, and NF-κB. Apigenin effectively downregulated the expression and secretion of pro-inflammatory cytokines through IL-23/IL-17/IL-22 axis. Apigenin suppressed nuclear translocation of NF-κB in LPS-induced RAW 264.7 cells. Cell migration and cell doubling assay in HaCaT cells showing the anti-proliferative potential of apigenin and it was found safe in acute dermal toxicity study. SIGNIFICANCE: Apigenin was found effective against psoriasis in both in-vitro and in-vivo models suggesting apigenin as a potential candidate for the development of anti-psoriatic agent.


Asunto(s)
Dermatitis , Psoriasis , Animales , Ratones , Humanos , Apigenina/farmacología , Apigenina/uso terapéutico , Células HaCaT/metabolismo , Células HaCaT/patología , FN-kappa B/metabolismo , Ratones Endogámicos BALB C , Lipopolisacáridos/farmacología , Células RAW 264.7 , Psoriasis/inducido químicamente , Queratinocitos/metabolismo , Antiinflamatorios/uso terapéutico , Dermatitis/tratamiento farmacológico , Dermatitis/patología , Inflamación/patología , Modelos Animales de Enfermedad
3.
Int J Pharm ; 643: 123212, 2023 Aug 25.
Artículo en Inglés | MEDLINE | ID: mdl-37429561

RESUMEN

Piperlongumine (PL) is a well-known bioactive alkaloid that has been reported as a potent anticancer molecule but has failed to provide potential activity in translational and clinical applications due to some drawbacks like low bioavailability, hydrophobicity, and rapid degradation. However, nano-formulation is a good choice to increase the bioavailability and enhance cellular uptake of PL. In this study, PL loaded nano-liposomes (NPL) were formulated using the thin-film hydration method and analyzed by Response Surface Methodology (RSM) in order to treat cervical cancer. The NPL were thoroughly characterized using particle size, PDI, zeta potential, drug loading capacity, encapsulation efficiency, SEM, AFM and FTIR. Different assays viz. MTT, AO/PI, DAPI, MMP, cell migration, DCFDA and apoptotic assay using Annexin V-FITC/PI were performed for anticancer potential of NPL in human cervical carcinoma cells (SiHa and HeLa). NPL showed enhanced cytotoxicity, diminished cell proliferation, reduced cell viability, enhanced nuclear condensation, reduction in mitochondrial membrane potential, inhibited cell migration, increased ROS level and promoted more apoptosis in both human cervical cancer cell lines. These findings demonstrated that NPL may be a potential therapeutic option for cervical cancer.


Asunto(s)
Antineoplásicos , Dioxolanos , Neoplasias del Cuello Uterino , Femenino , Humanos , Liposomas/farmacología , Neoplasias del Cuello Uterino/tratamiento farmacológico , Neoplasias del Cuello Uterino/patología , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Dioxolanos/farmacología , Apoptosis , Línea Celular Tumoral
4.
Oral Dis ; 2022 Dec 24.
Artículo en Inglés | MEDLINE | ID: mdl-36565439

RESUMEN

The aim of this review is to enumerate medicinal plants and their bioactive compounds that may become potential leads in the mitigation of oral submucous fibrosis (OSMF) in the forthcoming future. It is focused on pathophysiology, risk factors, current treatment regimen, potential plant leads, and future therapies for OSMF. Data were extracted from a vast literature survey by using SciFinder, Web of Science, Google Scholar, and PubMed search engines with relevant keywords. Upon literature survey, we found that the phytochemical 'arecoline' present in the areca nut is the main causative agent of OSMF condition. Currently, OSMF is treated by immunomodulatory and anti-inflammatory agents such as corticosteroids, enzymes (hyaluronidase, chymotrypsin, and collagenase), anti-inflammatory mediators (isoxsuprine and pentoxifylline), dietary supplements (vitamins, antioxidants, and micronutrients), and anti-fibrotic cytokines like interferon-gamma that provides short-term symptomatic relief to OSMF patients. However, some plant leads have been proven effective in alleviating symptoms and mitigating OSMF, which ultimately improves the quality of OSMF patients' life. We concluded that plant drugs like lycopene, curcumin, Aloe vera, colchicine, and Glycyrrhiza glabra are effective against OSMF in various in vitro and/or clinical studies and are being used by modern and traditional practitioners.

5.
Front Pharmacol ; 13: 913174, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35991888

RESUMEN

Introduction: Psoriasis is a chronic inflammatory skin disorder characterized by keratinocyte hyperproliferation and differentiation with increased immune cell infiltration. The anti-psoriatic effect of lavender oil has been reported. However, its phytoconstituents, linalool (L) and linalyl acetate (LA), showed a distinctive affinity with psoriasis targets. Objectives: This investigation was aimed to determine the combined effect of L and LA in ameliorating psoriasis-like skin inflammation and its safety in long-term topical uses. Methods: The combined effect of L and LA was compared with their individual effects. The anti-psoriatic activity was performed using imiquimod (IMQ)-induced psoriasis in BALB/c mice and evaluated to reduce PASI and CosCam scores and Th-1 and Th-17 cell-specific cytokine levels. The acute and repeated dose dermal toxicities were investigated as per the OECD guidelines. Results: L and LA combination (LLA) in the 1:1 w/w ratio at 2% concentration showed a synergistic effect. The combination showed 76.31% and 71.29% recovery in PASI and CosCam Scores; however, L2% and LA2% showed 64.28% and 47.61% recovery in PASI and 64.75 and 56.76% recovery in CosCam scores, respectively. It showed >90% and >100% recovery in Th-17 and Th-1 cell-specific cytokines, respectively, and restored epidermal hyperplasia and parakeratosis toward normal compared with psoriatic mice. A marked reduction in NF-κB, cck6, and the IL-17 expression was also observed in the LLA-treated group. This combination was safe in a therapeutically effective dose for 28 days as no significant changes were observed in organ and body weights, liver and kidney parameters, and differential leukocyte counts. Conclusion: This study proves the synergy between L and LA in a 1:1 w/w ratio at 2% in the treatment of psoriasis-like skin inflammation and provides strong scientific evidence for its safe topical use.

6.
Curr Top Med Chem ; 22(13): 1104-1133, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35642120

RESUMEN

BACKGROUND: Dandruff is a scalp disorder affecting the male populace predominantly. Topical agents and synthetic drugs used for dandruff treatment have specific side effects including burning at the application site, depression, dizziness, headache, itching or skin rash, nausea, stomach pain, vision change, vomiting, discoloration of hair, dryness or oiliness of the scalp and increased loss of hair. Thus, essential oils and extracts from plants could be valuable in the treatment and prevention of dandruff. AIMS & OBJECTIVES: This review aims to highlight current findings in dandruff occurrence, its etiology, promising plant essential oils/extracts, and novel treatment strategies. The main emphasis has been given on the anti-dandruff effect of essential oils and plant extracts to disrupt microbial growth. The proposed mechanism(s) of action, novel approaches used to perk up its biopharmaceutical properties, and topical application have been discussed. RESULTS: The literature survey was done, and bibliographic sources and research papers were retrieved from different search engines and databases, including SciFinder, PubMed, NCBI, Scopus, and Google Scholar. The selection of papers was accomplished based on exclusion and inclusion criteria. The scalp of diverse populations revealed an association of dandruff with microbial symbiosis, including Staphylococcus, Propionibacterium, Malassezia, and Candida as the pathogens responsible for the cause of dandruff. Topical antifungals are considered the first line of treatment for dandruff including azoles, with clotrimazole (1%), ketoconazole (2%), and miconazole (2%). Other commonly used therapies integrate benzoyl peroxide, coal tar, glycerin, zinc pyrithione, lithium succinate/gluconate, salicylic acid, selenium disulfide/sulfide, sodium sulfacetamide, etc. However, these medicaments and chemicals are known to cause specific side effects. Alternative therapies, including tea tree oil, thyme, Aloe vera, Mentha have been reported to demonstrate anti-dandruff activity by disrupting the microbial growth associated with dandruff formation. CONCLUSION: Overall, this review explains the occurrence of dandruff, its pathogenesis, and the potential applicability of promising plant essential oils/extracts and their novel treatment strategies. Further studies based on pre-clinical and clinical research are essential before making any conclusion about its efficacy in humans.


Asunto(s)
Caspa , Malassezia , Aceites Volátiles , Antifúngicos/farmacología , Caspa/tratamiento farmacológico , Caspa/microbiología , Humanos , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
7.
AAPS PharmSciTech ; 22(8): 259, 2021 Oct 26.
Artículo en Inglés | MEDLINE | ID: mdl-34704177

RESUMEN

Cliv-92 is a mixture of three structurally similar coumarinolignoids and a proven hepatoprotective agent. Low aqueous solubility and poor bioavailability are notable hindrances for its further use. Therefore, glycyrrhetinic acid-linked chitosan nanoparticles loaded with Cliv-92 were prepared for active targeting to the liver. The nanoparticles were prepared by the ionic gelation method to avoid the use of toxic solvents/rigorous agitation. The method of preparation was optimized using a central composite design with independent variables, namely polymer: drug ratio (3:1, w/w), crosslinker concentration (0.5%), and stirring speed (750 rpm). The optimized nanoparticles had a mean particle size of 185.17 nm, a polydispersity index of 0.41, a zeta potential of 30.93 mV, and a drug loading of 16.30%. The prepared formulation showed sustained release of approximately 63% of loaded Cliv-92 over 72 h. The nanoparticles were freeze-dried for long-term storage and further characterized. The formulation was found to be biocompatible for parenteral delivery. In vivo imaging study showed that optimized nanoparticles were preferentially accumulated in the liver and successfully targeting the liver. The present study successfully demonstrated the improved pharmacokinetic properties (≈12% relative bioavailability) and efficacy profile (evidenced by in vivo and histopathological studies) of fabricated Cliv-92 nanoparticles.


Asunto(s)
Quitosano , Ácido Glicirretínico , Nanopartículas , Portadores de Fármacos , Tamaño de la Partícula , Solubilidad
8.
Nat Prod Res ; 35(14): 2429-2432, 2021 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-31578883

RESUMEN

Chemical investigations on the stem of Cuscuta reflexa Roxb. (Convolvulaceae) led to the isolation of one new compound characterised as 3',4'-dimethoxy-1-phenyl-1α, 2-ethanediol (1), along with eight known compounds as tridecanyl palmitate, palmitic acid, n-pentatriacontane, n-triacont-21, 27-dien-1-ol, kaempherol, chlorogenic acid, 5,7-dimethoxyapigenin and quercitin. The chemical structures were established with the help of physical, chemical and spectroscopic methods. The antimicrobial potential of the new compound (1) was evaluated against three bacterial and three fungal pathogenic strain and showed significant activities.


Asunto(s)
Cuscuta/química , Fitoquímicos/farmacología , Tallos de la Planta/química , Antibacterianos/farmacología , Antifúngicos/farmacología , Espectroscopía de Resonancia Magnética con Carbono-13 , Pruebas de Sensibilidad Microbiana , Fitoquímicos/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Espectroscopía de Protones por Resonancia Magnética
9.
J Ethnopharmacol ; 261: 113127, 2020 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-32623016

RESUMEN

ETHNO-PHARMACOLOGICAL RELEVANCE: Lavender oil (LO) is an aromatic/essential oil extracted from Lavandula angustifolia and traditionally used as an aromatherapy massage oil due to its anti-inflammatory and wound healing property and also for providing the relief in other skin conditions such as psoriasis, dermatitis and eczema. However, LO has not been evaluated scientifically for psoriasis like skin inflammation. AIM OF THE STUDY: This study was aimed to investigate the LO and its major components linalool (L) and linalyl acetate (LA) against psoriasis like skin inflammation. MATERIALS AND METHODS: Anti-psoriatic activity was done using Imiquimod (IMQ) induced psoriasis like skin inflammation in BALB/c mice. Assessment of anti-psoriatic effect of LO, L and LA was done on the basis of change in ear thickness, psoriasis area severity index (PASI) scoring at alternative day, CosCam scoring using skin analyzer equipped with SkinSys software, biochemical, immunohistochemical and histological investigations. Level of effectiveness against psoriasis was investigated by percent reduction in PASI scores, CosCam scores and level of Th-1 and Th-17 cell expressing cytokines, as compared to the diseased mice. RESULTS: Topical application of LO 10% showed 73.67% recovery in PASI and 87% in Th-17 cell-specific cytokines towards normal as compared to disease group. L and LA were identified as the major components of LO and favoured ligands for selected psoriasis targets. At 2% topical dose, L and LA showed 64% and 47.61% recovery in PASI scores, respectively. Both, L and LA showed significant recovery in Th-1 specific TNF-α and IL-1ß however, only L showed significant recovery of Th-17 cytokines (IL-17 and IL-22). In contrast to LA (which restored granulosis), L restored epidermal hyperplasia and parakeratosis toward the normal condition. On the other hand, L also reduced the expression of NF-κß, ccr6 and IL-17, while LA reduced the expression of NF-κß only. At 10% topical dose, LO was observed to be slight irritant while at 2% topical dose, L and LA were found non-irritant to the skin. CONCLUSION: This study proves the effectiveness of LO and its major phytoconstituents linalool and linalyl acetate against IMQ induced psoriasis like skin inflammation and provides the scientific evidence for topical use of lavender oil.


Asunto(s)
Monoterpenos Acíclicos/farmacología , Fármacos Dermatológicos/farmacología , Lavandula , Monoterpenos/farmacología , Aceites Volátiles/farmacología , Aceites de Plantas/farmacología , Psoriasis/prevención & control , Piel/efectos de los fármacos , Monoterpenos Acíclicos/administración & dosificación , Monoterpenos Acíclicos/aislamiento & purificación , Administración Cutánea , Animales , Citocinas/metabolismo , Fármacos Dermatológicos/administración & dosificación , Fármacos Dermatológicos/aislamiento & purificación , Modelos Animales de Enfermedad , Femenino , Imiquimod , Mediadores de Inflamación/metabolismo , Lavandula/química , Ratones Endogámicos BALB C , Monoterpenos/administración & dosificación , Monoterpenos/aislamiento & purificación , Aceites Volátiles/administración & dosificación , Aceites Volátiles/aislamiento & purificación , Aceites de Plantas/administración & dosificación , Aceites de Plantas/aislamiento & purificación , Psoriasis/inducido químicamente , Psoriasis/metabolismo , Psoriasis/patología , Conejos , Transducción de Señal , Piel/metabolismo , Piel/patología
10.
J Control Release ; 270: 203-225, 2018 01 28.
Artículo en Inglés | MEDLINE | ID: mdl-29199062

RESUMEN

The use of nanoemulsion in augmenting dermal and transdermal effectiveness of drugs has now well established. The development of nanoemulsion based semisolid dosage forms is an active area of present research. However, thickening or liquid-to-semisolid conversion of the nanoemulsions provides opportunities to the formulation scientist to explore novel means of solving instability issues during transformation. Extending knowledge about the explicit role of nature/magnitude of zeta potential, types of emulsifiers and selection of appropriate semisolid bases could place these versatile carriers from laboratory to industrial scale. This article reviews the progressive advancement in the delivery of medicament via nanoemulsion with special reference to the dermal and transdermal administration. It is attempted to explore the most suitable semi solid dosage form for the particular type of nanoemulsion (o/w, w/o and others) and effect of particle size and zeta potential on the delivery of drugs through dermal or transdermal route. Finally, this review also highlights the basic principles and fundamental considerations of nanoemulsion manufacture, application of nanoemulsion based semisolid dosage forms in the dermal/transdermal administration and basic considerations during the nanoemulsion absorption into and through skin.


Asunto(s)
Portadores de Fármacos/administración & dosificación , Emulsiones/administración & dosificación , Nanoestructuras/administración & dosificación , Administración Cutánea , Animales , Química Farmacéutica , Estabilidad de Medicamentos , Humanos
11.
Pharmacogn Mag ; 13(Suppl 2): S316-S320, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28808399

RESUMEN

BACKGROUND: The paste of stem bark of Azadirachta indica (AI) has been traditionally used on wound and scar for rapid healing in Bundelkhand region of India. OBJECTIVE: In the present investigation, wound healing potential of different extracts of stem bark of AI was explored in mice model. MATERIALS AND METHODS: To study the wound healing properties in small animal model, the excision and incision wound models were used and water, ethanol-water (1:1, v/v) and ethanol extracts were applied topically (15% w/w in ointment base). In the excision wound model, wound contraction, hydroxyproline content, DNA content, protein content, and nitric oxide levels were estimated after 14 days of topical treatment along with histopathological examinations. In the incision wound model, wound breaking strength was determined after 10 days of topical application of different extracts of AI. RESULTS: The animals treated with water extract of AI exhibited significant increment in rate of wound contraction (93.39%, P < 0.01), hydroxyproline content (13.31 ± 6.65 mg/g of dry tissue, P < 0.001), DNA content (20.99 ± 0.68 µg/100 mg of tissue, P < 0.01), protein content (100.53 ± 7.88 mg/g of wet tissue, P < 0.01) and nitric oxide level (3.05 ± 0.03 mMol/g of tissue, P < 0.001) as well as in wound breaking strength (289.40 ± 29.45 g, P < 0.01) when compared with vehicle control group which was also supported by histopathological studies. CONCLUSION: The water extract of stem bark of AI possesses significant wound healing property, validating its traditional use.

12.
AAPS PharmSciTech ; 18(2): 381-392, 2017 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-27007741

RESUMEN

Andrographolide (AP), a phytoconstituent of Andrographis paniculata is reported as a potent hepatoprotective agent. However, utility of this molecule is restricted due to its low aqueous solubility, gastric instability and hence low bioavailability. It was aimed to formulate and characterize AP-loaded, natural biopolymer stabilized, multilayered nano-hydrocolloid delivery system. Nanoemulsion (NE) was formulated using layer-by-layer (LbL) technology via electrostatic deposition of chitosan over alginate encrusted o/w NE by ultra-sonication. Improved transparency and stability of NE were observed with increasing sonication time. Best stability was obtained after 20 min sonication and particle size of the multilayered NE was measured in the range of 90.8-167.8 nm. Transmission electron microscopy confirmed the progressive layering of nanosized NE. Higher magnitude of zeta potential (i.e., 22.9 to 31.01 mV) confirmed higher stability and coating of alginate layer over NE surface for the period of 3 months. NE showed strategic release pattern when assessed in vitro in various simulated biological fluids of GIT in timed pattern. Multilayered NE showed significant modulation in liver function test (ALT, ALP, AST, TBIL, DBIL, and liver glycogen) and serum cytokines (TNF-α, IL-6, IL-10, and IL-ß) when assessed in vivo in galactosamine-lipopolysaccharide intoxicated mice. In conclusion, the andrographolide engrained multi-layered NE enhanced the solubility, stability and henceforth assured the increased availability in simulated biological fluids. The in vivo study exhibited the significantly improved hepatoprotection by andrographolide when delivered in stable multi-layered NE carrier systems.


Asunto(s)
Coloides/química , Diterpenos/química , Hígado/diagnóstico por imagen , Nanopartículas/química , Polisacáridos/química , Sustancias Protectoras/química , Animales , Disponibilidad Biológica , Quitosano/química , Citocinas/sangre , Diterpenos/metabolismo , Diterpenos/farmacología , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Excipientes/química , Pruebas de Función Hepática/métodos , Masculino , Ratones , Tamaño de la Partícula , Sustancias Protectoras/metabolismo , Sustancias Protectoras/farmacología , Solubilidad
13.
AAPS PharmSciTech ; 17(4): 940-50, 2016 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26831445

RESUMEN

The present study aimed to develop buccoadhesive film of glimepiride with unique combination of polymers and to investigate its effect(s) on physicomechanical parameters, drug-release, and permeation of films. Drug-polymer interaction was examined by FTIR and DSC analysis. Films were prepared by solvent casting technique and characterized for film strength (320 ± 8.5 g, 28.98 ± 2.00 mJ), buccoadhesive strength (28.8 ± 1.37 g, 3.04 ± 0.32 mJ), and tensile strength (260 ± 6.88 g, 18.00 ± 0.44 mJ) by new instrumental techniques. Increase in polymer concentration augmented zeta potential of polymeric matrix-mucin mixture and exhibited strong buccoadhesion (electrical theory). Buccoadhesion was also influenced by particle size (adsorption theory) and swelling (wetting theory). Erosion behavior of films was observed in swelling and SEM studies. Film GM4 exhibited 98 ± 2% in vitro drug release and 85 ± 8% ex vivo drug permeation in 12 h with controlled diffusion mechanism. Films were compatible with oral probiotic microorganisms. Stability studies revealed no significant (P < 0.05) variation in physicomechanical characteristics.


Asunto(s)
Celulosa/administración & dosificación , Celulosa/química , Mucosa Bucal/metabolismo , Compuestos de Sulfonilurea/administración & dosificación , Compuestos de Sulfonilurea/química , Adhesividad , Administración Bucal , Animales , Disponibilidad Biológica , Difusión , Sistemas de Liberación de Medicamentos/métodos , Cabras , Tamaño de la Partícula , Permeabilidad , Polímeros/administración & dosificación , Polímeros/química , Resistencia a la Tracción
14.
Drug Dev Ind Pharm ; 42(9): 1434-45, 2016 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26821208

RESUMEN

PURPOSE: To develop and optimize nanoemulsion (NE)-based emulgel (EG) formulation as a potential vehicle for topical delivery of tea tree oil (TTO). METHODOLOGY: Central composite design was adopted for optimizing the processing conditions for NE preparation by high energy emulsification method viz. surfactant concentration, co-surfactant concentration, and stirring speed. The optimized NE was developed into emulgel (EG) using pH sensitive polymer Carbopol 940 and triethanolamine as alkalizer. The prepared EG was evaluated for its pH, viscosity, and texture parameters, ex vivo permeation at 37 °C and stability. Antimicrobial evaluation of EG in comparison to conventional gel and pure TTO was also carried out against selected microbial strains. RESULTS AND DISCUSSION: Optimized NE had particle size and zeta potential of 16.23 ± 0.411 nm and 36.11 ± 1.234 mV, respectively. TEM analysis revealed the spherical shape of droplets. The pH of EG (5.57 ± 0.05 ) was found to be in accordance with the range of human skin pH. EG also illustrated efficient permeation (79.58 µL/cm(2)) and flux value (JSS) of 7.96 µL cm(2)/h through skin in 10 h. Viscosity and texture parameters, firmness (9.3 ± 0.08 g), spreadability (2.26 ± 0.06 mJ), extrudability (61.6 ± 0.05 mJ), and adhesiveness (8.66 ± 0.08 g) depict its suitability for topical application. Antimicrobial evaluation of EG with same amount of TTO as conventional gel revealed broader zones of growth inhibitions against all the selected microbial strains. Moreover, EG was also found to be nonirritant (PII 0.0833). These parameters were consistent over 90 d. CONCLUSION: TTO EG turned out to be a promising vehicle for the topical delivery of TTO with enhanced therapeutic efficacy.


Asunto(s)
Polietilenglicoles/química , Polietileneimina/química , Aceite de Árbol de Té/química , Resinas Acrílicas/química , Administración Cutánea , Animales , Química Farmacéutica/métodos , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Estabilidad de Medicamentos , Emulsiones/administración & dosificación , Emulsiones/química , Excipientes/química , Humanos , Concentración de Iones de Hidrógeno , Nanogeles , Nanopartículas/administración & dosificación , Nanopartículas/química , Tamaño de la Partícula , Permeabilidad , Polietilenglicoles/administración & dosificación , Polietileneimina/administración & dosificación , Polímeros/química , Conejos , Piel/metabolismo , Absorción Cutánea , Tensoactivos/química , Aceite de Árbol de Té/administración & dosificación , Viscosidad
15.
Drug Deliv ; 23(7): 2371-2390, 2016 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-25544604

RESUMEN

CONTEXT: Existing medication systems for the treatment of diabetes mellitus (DM) are inconvenient and troublesome for effective and safe delivery of drugs to the specific site. Therefore, investigations are desired to deliver antidiabetics using novel delivery approaches followed by their commercialization. OBJECTIVE: The present review aims to provide a compilation on the latest development in the field of novel drug delivery systems (NDDSs) for antidiabetics with special emphasis on particulate, vesicular and miscellaneous systems. METHODS: Review of literature (restricted to English language only) was done using electronic databases like Pubmed® and Scirus, i.e. published during 2005-2013. The CIMS/MIMS India Medical Drug Information eBook was used regarding available marketed formulation of antidiabetic drugs. Keywords used were "nanoparticle", "microparticle", "liposomes", "niosomes", "transdermal systems", "insulin", "antidiabetic drugs" and "novel drug delivery systems". Single inclusion was made for one article. If in vivo study was not done then article was seldom included in the manuscript. RESULTS: The curiosity to develop NDDSs of antidiabetic drugs with special attention to the nanoparticulate system followed by microparticulate and lipid-based system is found to emerge gradually to overcome the problems associated with the conventional dosage forms and to win the confidence of end users towards the higher acceptability. CONCLUSION: In the current scientific panorama when the area of novel drug delivery system has been recognized for its palpable benefits, unique potential of providing physical stability, sustained and site-specific drug delivery for a scheduled period of time can open new vistas for precise, safe and quality treatment of DM.


Asunto(s)
Diabetes Mellitus/tratamiento farmacológico , Sistemas de Liberación de Medicamentos/métodos , Hipoglucemiantes/farmacología , Liposomas/química , Nanopartículas/química , Humanos , Hipoglucemiantes/química , Liposomas/metabolismo
16.
AAPS PharmSciTech ; 17(2): 482-92, 2016 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-26248538

RESUMEN

Mentha spicata L. var. viridis oil (MVO) is a potent antifungal agent, but its application in the topical treatment is limited due to its irritancy and volatility. It was aimed to develop more efficient, chitosan-incrusted MVO microspheres with reduced volatility and lesser irritancy and to dispense it in the form of ointment. Simple coacervation technique was employed to microencapsulate MVO in chitosan matrix. Morphological properties and polymer cross-linking were characterized by scanning electron microscopy and differential scanning calorimetry, respectively. Optimization was carried out on the basis of entrapment efficiency (EE) using response surface methodology. Well-designed microspheres having smooth surface and spherical shape were observed. EE (81.20%) of optimum batch (R21) was found at 1.62% w/v of cross-linker, 5.4:5 of MVO to chitosan ratio and at 1000 rpm. R21 showed 69.38 ± 1.29% in vitro MVO release in 12 h and 96.92% retention of MVO in microspheres even after 8 week. Ointments of PEG 4000 and PEG 400 comprising MVO (F1) and R21 (F2) were developed separately. F2 showed comparatively broader zone of growth inhibition (13.33 ± 1.76-18.67 ± 0.88 mm) and less irritancy (PII 0.5833, irritation barely perceptible) than that of F1. F2 was able to avoid the direct contact of mild irritant MVO with the skin and to reduce its rapid volatility. Controlled release of MVO helped in lengthening the duration of availability of MVO in agar media and hence improved its therapeutic efficacy. In conclusion, a stable and non-irritant formulation with improved therapeutic potential was developed.


Asunto(s)
Quitosano/química , Mentha/química , Aceites de Plantas/administración & dosificación , Aceites de Plantas/química , Polímeros/química , Piel/efectos de los fármacos , Administración Tópica , Animales , Rastreo Diferencial de Calorimetría/métodos , Química Farmacéutica/métodos , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/química , Composición de Medicamentos/métodos , Femenino , Masculino , Microscopía Electrónica de Rastreo/métodos , Microesferas , Pomadas/administración & dosificación , Pomadas/química , Tamaño de la Partícula , Conejos , Piel/microbiología
17.
Biomed Res Int ; 2014: 786084, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-25379509

RESUMEN

Citronella essential oil (CEO) has been reported as an excellent mosquito repellent; however, mild irritancy and rapid volatility limit its topical application. It was aimed to develop a nonirritant, stable, and consistent cream of CEO with improved residence time on skin using an industrial approach. Phase inversion temperature technique was employed to prepare the cream. It was optimized and characterized based on sensorial evaluation, emulsification, and consistency in terms of softness, greasiness, stickiness, and pH. The optimum batch (B5) was evaluated for viscosity (90249.67±139.95 cP), texture profile with respect to firmness (38.67±0.88 g), spreadability (70.33±0.88 mJ), and extrudability (639.67±8.09±0.1 mJ) using texture analyzer along with two most popular marketed products selected as reference standard. Subsequently, B5 was found to be stable for more than 90 days and showed enhanced duration of mosquito repellency as compared to CEO. HS-GC ensured the intactness of CEO in B5. Investigated primary irritation index (PII 0.45) positioned B5 into the category of irritation barely perceptible. The pronounced texture profile and stability of B5 with extended residence time and less PII revealed its potential application in industry and offered a promising alternative to the marketed products of synthetic origin.


Asunto(s)
Química Farmacéutica , Repelentes de Insectos/uso terapéutico , Aceites de Plantas/uso terapéutico , Crema para la Piel/uso terapéutico , Animales , Culicidae/efectos de los fármacos , Humanos , Repelentes de Insectos/química , Aceites de Plantas/química , Crema para la Piel/química
18.
Biomed Res Int ; 2014: 301304, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-25147793

RESUMEN

Acne is a common but serious skin disease, which affects approximately 80% adolescents and young adults in 11-30 age group. 42.5% of men and 50.9% of women continue to suffer from this disease into their twenties. Bacterial resistance is now at the alarming stage due to the irrational use of antibiotics. Hence, search for new lead molecule/bioactive and rational delivery of the existing drug (for better therapeutic effect) to the site of action is the need of the hour. Plants and plant-derived products have been an integral part of health care system since time immemorial. Therefore, plants that are currently used for the treatment of acne and those with a high potential are summarized in the present review. Most active plant extracts, namely, P. granatum, M. alba, A. anomala, and M. aquifolium exhibit minimum inhibitory concentration (MIC) in the range of 4-50 µg/mL against P. acnes, while aromatic oils of C. obovoides, C. natsudaidai, C. japonica, and C. nardus possess MICs 0.005-0.6 µL/mL and phytomolecules such as rhodomyrtone, pulsaquinone, hydropulsaquinone, honokiol, magnolol, xanthohumol lupulones, chebulagic acid and rhinacanthin-C show MIC in the range of 0.5-12.5 µg/mL. Novel drug delivery strategies of important plant leads in the treatment of acne have also been discussed.


Asunto(s)
Acné Vulgar/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Plantas Medicinales/química , Antibacterianos/uso terapéutico , Humanos , Fitoterapia/métodos
19.
ScientificWorldJournal ; 2014: 406921, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24688387

RESUMEN

In North India, poultice of young unfolded leaves of Argyreia speciosa Linn. (Convolvulaceae) is used for healing wounds. In order to find scientific evidence for the traditional utilization of leaves of A. speciosa in wound healing, this investigation was carried out. A linear incision wound of about 3 cm in length and 2 mm in depth and circular excision wound of 177 mm(2) full thickness were made on the dorsal region of separate groups (n = 5) of anesthetized Swiss albino mice. A simple ointment, developed by including ethanol, ethanol-water, and water extracts (10% each, separately) of A. speciosa, was applied topically to mice once daily for 14 days after wounding. To evaluate the effect of each extract, wound contraction, epithelization period, wound breaking strength, and hydroxyproline content were determined. The water extract of A. speciosa showed accelerated wound healing activity as evidenced by fast wound contraction (96.30 ± 0.52%; P < 0.01), rapid epithelization period (11.40 ± 0.60 days; P < 0.001), greater wound breaking strength (376.56 ± 21.16 g; P < 0.001), and higher hydroxyproline content (16.49 ± 1.12 mg/g; P < 0.05) of granulation tissue. The present report supports the traditional use of Argyreia speciosa leaves for wound healing and signify its relevant therapeutic potential.


Asunto(s)
Ipomoea/química , Extractos Vegetales/administración & dosificación , Hojas de la Planta/química , Cicatrización de Heridas/efectos de los fármacos , Cicatrización de Heridas/fisiología , Heridas Penetrantes/tratamiento farmacológico , Heridas Penetrantes/patología , Administración Tópica , Animales , Masculino , Ratones , Resultado del Tratamiento , Heridas Penetrantes/fisiopatología
20.
Carbohydr Polym ; 103: 126-33, 2014 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-24528709

RESUMEN

Aim of the present investigation was to develop cellulosic polymer based mucoadhesive antifungal gel comprising novel ternary mixture of miconazole nitrate (MN) for buccal delivery. Crosslinking of gel was made by adjusting pH with triethanolamine (TEA) and gel formulation was optimized on the basis of flux of MN (0.562-1.751 mg/cm(2)/h) calculated from ex vivo permeation study. Based on statistically validated polynomial equation and plotted response surfaces, B17 was found to be the optimum batch. Texture profile in terms of adhesiveness (3.24 ± 0.012 g), firmness (10.83 ± 0.067 g), spreadability (3.63 ± 0.033 mJ) and extrudability (35.6 ± 0.1 mJ) of B17 was evaluated using a novel instrumental approach. The texture parameters were found to be consistent over 90 days. Ternary mixture containing gel showed broader zone of growth inhibition (32.67-47.33 mm) in comparison to marketed formulation containing pure MN (17.50-40.33 mm) against selected strains of fungi. In conclusion, consistent and effective mucoadhesive antifungal gel of MN with extended residence time in oral mucosa was developed.


Asunto(s)
Antifúngicos/farmacología , Celulosa/farmacología , Sistemas de Liberación de Medicamentos , Geles/farmacología , Miconazol/química , Polímeros/farmacología , Antifúngicos/síntesis química , Antifúngicos/química , Candida albicans/efectos de los fármacos , Celulosa/síntesis química , Celulosa/química , Cryptococcus neoformans/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Geles/síntesis química , Geles/química , Pruebas de Sensibilidad Microbiana , Polímeros/síntesis química , Polímeros/química , Sporothrix/efectos de los fármacos , Relación Estructura-Actividad
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