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Chronic lung diseases such as asthma, chronic obstructive pulmonary disease, lung cancer, and the recently emerged COVID-19, are a huge threat to human health, and among the leading causes of global morbidity and mortality every year. Despite availability of various conventional therapeutics, many patients remain poorly controlled and have a poor quality of life. Furthermore, the treatment and diagnosis of these diseases are becoming increasingly challenging. In the recent years, the application of nanomedicine has become increasingly popular as a novel strategy for diagnosis, treatment, prevention, as well as follow-up of chronic lung diseases. This is attributed to the ability of nanoscale drug carriers to achieve targeted delivery of therapeutic moieties with specificity to diseased site within the lung, thereby enhancing therapeutic outcomes of conventional therapies whilst minimizing the risks of adverse reactions. For this instance, monoolein is a polar lipid nanomaterial best known for its versatility, thermodynamic stability, biocompatibility, and biodegradability. As such, it is commonly employed in liquid crystalline systems for various drug delivery applications. In this review, we present the applications of monoolein as a novel nanomaterial-based strategy for targeted drug delivery with the potential to revolutionize therapeutic approaches in chronic lung diseases.
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Carbon nanotubes (CNTs), owing to their inherently unique properties in the domain of biomedical sciences including drug delivery, offer an exciting platform to the researchers. Of late, their applications have also been successfully established. Recently, single-walled CNTs (SWCNTs) have been explored for antibacterial efficacy, but naïve multi-walled CNTs (MWCNTs) still remained unearthed. The present studies endeavor the investigation of the potential of various non-ionic surfactants in solubility enhancement of MWCNTs and their subsequent antibacterial efficacy against Escherichia coli and Staphylococcus aureus. Polysorbates offer more solubility to MWCNTs vis-à-vis the phospholipids. However, the antibacterial effect was found to be less influenced by solubility but significantly determined by the type of surfactant. Transmission electron photomicrographs confirmed significant adhesion of MWCNTs to the bacterial walls only in the presence of unsaturated phospholipids and this was expressed in the form of lowest minimum inhibitory concentration (MIC) values of MWCNTs dispersed with the same. The findings are unique as MWCNTs were found to be active against both Gram-negative and Gram-positive bacteria to a similar extent, though somewhat milder than SWCNTs. However, when dispersed with unsaturated phospholipids, the former offer almost comparable antibacterial effects to that of the latter. The study opens a new research domain to further explore the antibacterial effects of non-functionalized and relatively safer MWCNTs, accentuating the importance of biocomponents like unsaturated phospholipids in this purview.
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Antibacterianos/química , Antibacterianos/farmacologia , Nanotubos de Carbono/química , Parede Celular/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana/métodos , Fosfolipídeos/química , Staphylococcus aureus/efeitos dos fármacos , Tensoativos/químicaRESUMO
OBJECTIVE: Tamoxifen (TAM) is widely employed in the treatment of breast malignancies and is also found to be effective in psoriasis treatment. The current studies aimed to explore the antipsoriatic potential of topical TAM encapsulated in the new generation phospholipid-based vesicular and micellar systems, i.e. flexible membrane vesicles (FMVs) and pluronic lecithinized organogels (PLOs). METHODS: TAM-loaded-FMVs were prepared by thin-film hydration technique, while TAM-PLOs were prepared by simple mixing. Mouse-tail model was used to evaluate the antipsoriatic activity of the novel formulations. The mouse tails were treated once-a-day with different formulations for a period of four weeks and prepared for longitudinal histological sections by hematoxylin-eosin staining technique. The length of the orthokeratotic regions in stratum granulosum was measured on 10 sequential scales per tail section as percentage of the full length of the scale, and the drug activity was calculated further. RESULTS: Evaluation of antipsoriatic activity on mice tail revealed significantly higher (p < 0.01) efficacy of TAM-FMV gel (i.e. 35.8%) and TAM-PLO (i.e. 24.6%) vis-à-vis the conventional TAM-hydrogel (i.e. 10.2%). CONCLUSIONS: The results of these studies demonstrated immense potential of the topically applied TAM-encapsulated vesicular and micellar systems in psoriasis, thus calling for more comprehensive investigations to establish the role of TAM in the management of psoriasis.
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Antineoplásicos Hormonais/administração & dosagem , Lipossomos/química , Micelas , Fosfolipídeos/química , Psoríase/tratamento farmacológico , Tamoxifeno/administração & dosagem , Administração Tópica , Animais , Antineoplásicos Hormonais/uso terapêutico , Modelos Animais de Doenças , Feminino , Géis/química , Géis/metabolismo , Lecitinas/química , Lecitinas/metabolismo , Lipossomos/metabolismo , Camundongos , Fosfolipídeos/metabolismo , Psoríase/patologia , Pele/efeitos dos fármacos , Pele/patologia , Tamoxifeno/uso terapêuticoRESUMO
The eye is a most delicate organ protected by several complex biological barriers that are static and dynamic. The presence of these ocular barriers retards drug absorption from topically applied dosage forms at the conjunctival sac. The efficient topical delivery of the drug into the globe is more difficult to achieve and there is a need to develop a topical formulation that may reduce the use of injections and increase patient compliance with decreased frequency of administration. In the advancements of research in nanotechnology, nanoemulsions can be used as biocompatible carriers to deliver the drug to the ocular cavity. The lipophilic globules can increase the solubility of hydrophobic cargos which provides increased permeation ability and ocular bioavailability which can sustain drug release and corneal retention. Because of their small size, these formulations do not cause blurring of vision. Nanoemulsions (NEs) over the past decade have been used to treat several ocular diseases in the anterior eye segment. This review summarizes the economic burden, pathology of ocular diseases, formulation considerations for ocular formulations, and recent advances of these NEs as effective carriers for ocular drug delivery highlighting their performance in pre-clinical studies.
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Acne, a common skin disease in teenagers, is caused by Propionibacterium acnes (P. acnes). Isotretinoin (ITR) is though reported to have immense antiacne potential, yet there are hardly any reports vouching its antimicrobial activity. The present study, therefore, was undertaken to study the antimicrobial activity of ITR and evaluate the effect of its encasement in nanocarriers on its minimum inhibitory concentration (MIC). The nanocarriers were also evaluated for the skin transport characteristics. MICs of pure drug and entrapped drug in nanolipid carriers (ITR-NLCs) and in solid lipid nanoparticles (ITR-SLNs) were determined by broth dilution method against clindamycin phosphate as the reference antibiotic. It was observed that ITR possessed marked antimicrobial activity against anaerobic pathogen, P. acnes. Nanocarriers loaded with ITR, that is, SLNs and NLCs, enhanced the antimicrobial activity even at lower concentrations vis-à-vis the drug alone and improved drug transport potential vis-à-vis the commercial gel. The unique findings could be the result of effective adhesion of ITR-loaded nanocarriers to the bacterial membranes and release of drug directly to the target. Besides establishing ITR as an antimicrobial agent against acne-causing bacteria, the current work ratifies immense potential of nanocolloidal carriers like SLNs and NLCs to treat acne in a more efficient manner.
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Fármacos Dermatológicos/administração & dosagem , Fármacos Dermatológicos/farmacocinética , Isotretinoína/administração & dosagem , Isotretinoína/farmacocinética , Propionibacterium acnes/efeitos dos fármacos , Acne Vulgar/tratamento farmacológico , Acne Vulgar/microbiologia , Animais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/farmacocinética , Portadores de Fármacos/química , Humanos , Lipídeos/química , Masculino , Camundongos , Camundongos Pelados , Modelos Biológicos , Nanocápsulas/administração & dosagem , Nanocápsulas/química , Nanocápsulas/ultraestrutura , Nanopartículas/administração & dosagem , Nanopartículas/química , Nanopartículas/ultraestrutura , Permeabilidade , Propionibacterium acnes/patogenicidade , Ratos , Ratos Wistar , Pele/metabolismoRESUMO
A diabetic foot ulcer is a chronic clinical manifestation of diabetes that exacerbates the condition of a patient and has a considerable socioeconomic impact. A diabetic foot ulcer (DFU) impacts around 25% of patients with diabetes mellitus at a certain point in their lives, and the underlying cause of the condition appears to be linked to neuropathic, ischaemic, and/or neuroischaemic pathologies. For the effective treatment of DFU, a variety of conventional treatments are used. However, in recent years, a range of innovative materials have been studied to bolster standard treatment tactics and promote the desired biological response by transcending the impediments of current wound healing approaches. Inorganic/organic hydrogel hybrids for tissue regeneration are among the most promising materials. This review article outlines the current treatment options for DFU, applications of hydrogel with an emphasis on wound healing, polymeric materials used to fabricate hydrogel, and the role of emerging technologies.
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Diabetes Mellitus , Pé Diabético , Humanos , Hidrogéis/uso terapêutico , Pé Diabético/tratamento farmacológico , Cicatrização , Resultado do Tratamento , PolímerosRESUMO
Cancer is characterized by disrupted molecular variables caused by cells that deviate from regular signal transduction. The uncontrolled segment of such cancerous cells annihilates most of the tissues that contact them. Gene therapy, immunotherapy, and nanotechnology advancements have resulted in novel strategies for anticancer drug delivery. Furthermore, diverse dispersion of nanoparticles in normal stroma cells adversely affects the healthy cells and disrupts the crosstalk of tumour stroma. It can contribute to cancer cell progression inhibition and, conversely, to acquired resistance, enabling cancer cell metastasis and proliferation. The tumour's microenvironment is critical in controlling the dispersion and physiological activities of nano-chemotherapeutics which is one of the targeted drug therapy. As it is one of the methods of treating cancer that involves the use of medications or other substances to specifically target and kill off certain subsets of malignant cells. A targeted therapy may be administered alone or in addition to more conventional methods of care like surgery, chemotherapy, or radiation treatment. The tumour microenvironment, stromatogenesis, barriers and advancement in the drug delivery system across tumour tissue are summarised in this review.
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COVID-19 remains a life-threatening infectious disease worldwide. Several bio-active agents have been tested and evaluated in an effort to contain this disease. Unfortunately, none of the therapies have been successful, owing to their safety concerns and the presence of various adverse effects. Various countries have developed vaccines as a preventive measure; however, they have not been widely accepted as effective strategies. The virus has proven to be exceedingly contagious and lethal, so finding an effective treatment strategy has been a top priority in medical research. The significance of vitamin D in influencing many components of the innate and adaptive immune systems is examined in this study. This review aims to summarize the research on the use of vitamin D for COVID-19 treatment and prevention. Vitamin D supplementation has now become an efficient option to boost the immune response for all ages in preventing the spread of infection. Vitamin D is an immunomodulator that treats infected lung tissue by improving innate and adaptive immune responses and downregulating the inflammatory cascades. The preventive action exerted by vitamin D supplementation (at a specific dose) has been accepted by several observational research investigations and clinical trials on the avoidance of viral and acute respiratory dysfunctions. To assess the existing consensus about vitamin D supplementation as a strategy to treat and prevent the development and progression of COVID-19 disease, this review intends to synthesize the evidence around vitamin D in relation to COVID-19 infection.
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COVID-19 , Humanos , COVID-19/prevenção & controle , Vitamina D/uso terapêutico , Tratamento Farmacológico da COVID-19 , SARS-CoV-2 , Suplementos Nutricionais/efeitos adversos , Fatores Imunológicos/efeitos adversos , Adjuvantes ImunológicosRESUMO
Diabetic retinopathy (DR) is one of the chronic complications of diabetes. It includes retinal blood vessels' damage. If untreated, it leads to loss of vision. The existing treatment strategies for DR are expensive, invasive, and need expertise during administration. Hence, there is a need to develop a non-invasive topical formulation that can penetrate deep to the posterior segment of retina and treat the damaged retinal vessels. In addition, it should also provide sustained release. In recent years, novel drug delivery systems (NDDS) have been explored for treating DR and found successful. In this study, chitosan (CS) modified 5-Fluorouracil Nanostructured Lipid Carriers (CS-5-FU-NLCs) were prepared by modified melt emulsification-ultrasonication method and optimized by Box-Behnken Design. The size, polydispersity index, zeta potential and entrapment efficiency of CS-5-FU-NLCs were 163.2 ± 2.3 nm, 0.28 ± 1.52, 21.4 ± 0.5 mV and 85.0 ± 0.2 %, respectively. The in vitro drug release and ex vivo permeation study confirmed higher and sustained drug release in CS-5-FU-NLCs as compared to 5-FU solution. HET-CAM Model ensured the non-irritant nature of CS-5-FU-NLCs. In vivo ocular studies of CS-5-FU-NLCs confirmed antiangiogenic effect of 5-FU by CAM model and diabetic retinopathy induced rat model, indicating successful delivery of 5-FU to the retina.
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Antineoplásicos , Quitosana , Diabetes Mellitus , Retinopatia Diabética , Nanoestruturas , Ratos , Animais , Fluoruracila , Portadores de Fármacos , Lipídeos , Tamanho da Partícula , Liberação Controlada de FármacosRESUMO
Pharmaceutical oral dosage forms are tremendously preferred by both consumers as well as pharmaceutical manufacturers owing to the plethora of benefits they offer. Lozenges (LZs) are one of the dosage forms that provide a palatable means of drug administration and have great importance with respect to their pharmaceutical applications. LZs offer additional benefits to pediatric and geriatric patients, along with people having problems associated with the gastro-intestinal tract. Dysphagia is a common problem faced by all age groups, which gives rise to the need for LZs. Moreover, the foremost merit presented by the medicated LZs includes its augmented retention time in the oral cavity that results in an enhanced bioavailability for buccal or upper gastro-intestinal disorders. Further, LZs can also be used to bypass the first-pass effect. The present review covers various aspects of LZs such as formulation, manufacturing techniques, evaluation parameters, marketed products, patents, and a compilation of research work that has been done on lozenges as a delivery system.
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Boca , Idoso , Disponibilidade Biológica , Criança , Humanos , ComprimidosRESUMO
INTRODUCTION: Non-aqueous nano-emulsions (NANEs) are colloidal lipid-based dispersions with nano-sized droplets formed by mixing two immiscible phases, none of which happens to be an aqueous phase. Their ability to incorporate water and oxygen sensitive drugs without any susceptibility to degradation makes them the optimum dosage form for such candidates. In NANEs, polar liquids or polyols replace the aqueous phase while surfactants remain same as used in conventional emulsions. They are a part of the nano-emulsion family albeit with substantial difference in composition and application. AREAS COVERED: The present review provides a brief insight into the strategies of loading water-sensitive drugs into NANEs. Further advancement in these anhydrous systems with the use of solid particulate surfactants in the form of Pickering emulsions is also discussed. EXPERT OPINION: NANEs offer a unique platform for delivering water-sensitive drugs by loading them in anhydrous formulation. The biggest advantage of NANEs vis-à-vis the other nano-cargos is that they can also be prepared without using equipment-intensive techniques. However, the use of NANEs in drug delivery is quite limited. Looking at the small number of studies available in this direction, a need for further research in this field is required to explore this delivery system further.
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Tensoativos , EmulsõesRESUMO
Liquid self-nanoemulsifying drug delivery system (L-SNEDDS) of curcumin and quercetin were prepared by dissolving them in isotropic mixture of Labrafil M1944CS®, Capmul MCM®, Tween-80® and Transcutol P®. The prepared L-SNEDDS were solidified using Ganoderma lucidum extract, probiotics and Aerosil-200® using spray drying. These were further converted into pellets using extrusion-spheronization. The mean droplet size and zeta potential of L-SNEDDS were found to be 63.46 ± 2.12 nm and - 14.8 ± 3.11 mV while for solid SNEDDS pellets, these were 72.46 ± 2.16 nm and -38.7 ± 1.34 mV, respectively. The dissolution rate for curcumin and quercetin each was enhanced by 4.5 folds while permeability was enhanced by 5.28 folds (curcumin) and 3.35 folds (quercetin) when loaded into SNEDDS pellets. The Cmax for curcumin and quercetin containing SNEDDS pellets was found 532.34 ± 5.64 ng/mL and 4280 ± 65.67 ng/mL, respectively. This was 17.55 and 3.48 folds higher as compared to their naïve forms. About 50.23- and 5.57-folds increase in bioavailability was observed for curcumin and quercetin respectively, upon loading into SNEDDS pellets. SNEDDS pellets were found stable at accelerated storage conditions. The developed formulation was able to normalize the levels of blood glucose, lipids, antioxidant biomarkers, and tissue architecture of pancreas and liver in streptozotocin induced diabetic rats as compared to their naïve forms.
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Curcumina , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Nanopartículas , Probióticos , Reishi , Administração Oral , Animais , Disponibilidade Biológica , Diabetes Mellitus Experimental/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Emulsões , Tamanho da Partícula , Pós/uso terapêutico , Quercetina/uso terapêutico , Ratos , Solubilidade , EstreptozocinaRESUMO
Synbiotics, are a combination of probiotics and prebiotics. They play an important role in metabolizing different nutritional substrates and thus helps in the maintenance of human health. Any disbalance in the gut microflora, known as dysbiosis, is known to lead to a number of diseased conditions. It can be reverted by the administration of synbiotics. Present review highlights various mechanistic pathways through which synbiotics act as therapeutics. The dual role of synbiotics as nutraceutical and excipient in developing oral formulations are entailed with case studies. The findings entailed that there exist numerous studies on prebiotics as well as probiotics have been carried out to show their effects in several diseases. However, the concept of combining together them for prevention and treatment of various pathological conditions accruing from dysbiosis is relatively new. Synbiotics, however, face challenge of low stability during their sojourn in the GIT, which is generally overcome by various encapsulation techniques. Various studies also showed potential role of synbiotics in drug delivery. However, it is an emerging area and lacks clinical correlation. It is important to focus on clinical trials of formulations wherein synbiotics have been used as therapeutic moiety as well as pharmaceutical carrier for treating various diseases.
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Probióticos , Simbióticos , Humanos , Prebióticos , Disbiose , Excipientes , Probióticos/farmacologia , Probióticos/uso terapêuticoRESUMO
Non-aqueous nanoemulsion (NANE) of Alpinia galanga extract (AGE) was prepared using Palmester 3595 (MCT oil) as oil phase, Cremophor RH 40-Transcutol P® as surfactant-co-surfactant (Smix), and glycerin as non-aqueous polar continuous phase. The composition was optimized by applying three-level, four factor Box-Behnken design (BBD). The mean droplet size and zeta potential of the optimized AGE NANE was found to be 60.81 ± 18.88 nm and -7.99 ± 4.14 mV, respectively. The ex vivo permeation studies of AGE NANE and AGE per se on porcine skin reported flux of 125.58 ± 8.36 µg/cm2 h-1 and 12.02 ± 1.64 µg/cm2 h-1, respectively. Therefore, the enhancement ratio has shown 10-folds increase in the flux for AGE NANE when compared to extract per se. Later, confocal laser scanning microcopy confirmed that AGE NANE were able to penetrate into skin's stratum by trans-follicular transport mechanism. The stability studies of AGE NANE confirmed its stability at 30 ± 2 °C/75 ± 5 % RH and 5 ± 3 °C. The efficacy of AGE NANE was evaluated in vivo on imiquimod (IMQ) induced mouse model. The mice treated with low and high doses of AGE NANE (groups VI and VII) showed significant (p < 0.05) amelioration of psoriasis. Results of histopathology indicated reduction in psoriasis area severity index in AGE NANE treated mice (group VI and group VII).
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Alpinia , Nanopartículas , Psoríase , Administração Cutânea , Animais , Emulsões , Camundongos , Psoríase/tratamento farmacológico , Absorção Cutânea , Tensoativos , SuínosRESUMO
ETHANOPHARMACOLOGICAL IMPORTANCE: Alpinia galanga (L.) Willd (AG), belonging to Zingiberaceae family is used as a spice and condiment in various culinary preparations of Indonesia, Thailand and Malaysia. It has been also used as a key ingredient in various traditional systems of medicine for the treatment of throat infection, asthma, urinary ailments, inflammation and rheumatism amongst other conditions. AG is widely used as a functional food and included in various preparations to obtain its nutraceutical and pharmacological benefits of its phytoconstituents such as phenyl propanoids, flavonoids and terpenoids. Over the past decades, several researchers have carried out systematic investigation on various parts of AG. Numerous studies on AG rhizomes have shown positive pharmacological effects such as anti-inflammatory, anticancer, antipsoriasis, antiallergic, neuroprotective and thermogenesis. Till date, no comprehensive review summarizing the exploitation of AG into nanomedicine has been published. AIM OF THE REVIEW: This comprehensive review aims to briefly discuss cultivation methods, propagation techniques, extraction processes for AG. The ethnopharmacological uses and pharmacological activities of AG extracts and its isolates are discussed in detail which may contribute well in further development of novel drug delivery system (NDDS) i.e. future nanomedicine. MATERIALS AND METHODS: Information about AG was collected using search engine tools such as Google, Google Scholar, PubMed, Google Patent, Web of Science and bibliographic databases of previously published peer-reviewed review articles and research works were explored. The obtained data sets were sequentially arranged for better understanding of AG's potential. RESULTS: More advanced genetic engineering techniques have been utilized in cultivation and propagation of AG for obtaining better yield. Extraction, isolation and characterization techniques have reported numerous phytoconstituents which are chemically phenolic compounds (phenyl propanoids, flavonoids, chalcones, lignans) and terpenes. Ethnopharmacological uses and pharmacological activity of AG are explored in numerous ailments, their mechanism of action and its further potential to explore into novel drug delivery system are also highlighted. CONCLUSIONS: The review highlights the importance of plant tissue culture in increasing the production of AG plantlets and rhizomes. It was understood from the review that AG and its phytoconstituents possess numerous pharmacological activities and have been explored for the treatment of cancer, microbial infection, gastrointestinal disorders, neuroprotective effects, obesity and skin disorders. However, the use of AG as alternative medicine is limited owing to poor solubility of its bioactive components and their instability. To overcome these challenges, novel drug delivery systems (NDDS) have been utilized and found good success in overcoming its aforementioned challenges. Furthermore, efforts are required towards development of scalable, non-toxic and stable NDDS of AG and/or its bioactives.
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Alpinia , Suplementos Nutricionais , Etnofarmacologia/métodos , Medicina Tradicional/métodos , Nanomedicina , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , EspeciariasRESUMO
BACKGROUND AND OBJECTIVE: Psoriasis is an autoimmune skin disease involving cascading release of cytokines activated by the innate and acquired immune system. The increasing prevalence rate of psoriasis demands for more appropriate therapy. The existing chemical moiety is promising for better therapeutic outcome, but the selection of a proper channel for administration has to be reviewed. Hence there is a need to select the most appropriate dosage form and route of administration for improving the curative rate of psoriasis. RESULTS: A total of 108 systematic reviews of research and review articles were conducted to make the manuscript comprehensible. The role of inflammatory mediators in the pathogenesis of the disease is discussed for a better understanding of the selection of pharmacotherapy. The older and newer therapeutic moiety with its mode of administration for psoriasis treatment has been discussed. With a comparative review on topical and oral administration of first-line drugs such as methotrexate (MTX), cyclosporine (CsA), and betamethasone, its benefits-liabilities in the selected routes were accounted for. Emphasis has also been paid on advanced nanocarriers for dermatologic applications. CONCLUSION: For a better therapeutic outcome, proper selection of drug moiety with its appropriate administration is the major requisite. With the advent of nanotechnology, the development of nanocarrier for dermatologic application has been successfully demonstrated in positioning the systemically administrated drug into topical targeted delivery. In a nutshell, to achieve successful treatment strategies towards psoriasis, there is a need to focus on the development of stable, non-toxic nanocarrier for topical delivery. Inclusion of the existing orally administered drug moiety into nanocarriers for topical delivery is proposed in order to enhance therapeutics payload with reduced side effects which serves as a better treatment approach for relief of the psoriasis condition.
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Fármacos Dermatológicos/administração & dosagem , Portadores de Fármacos , Nanopartículas , Psoríase/tratamento farmacológico , Pele/efeitos dos fármacos , Administração Cutânea , Animais , Citocinas/metabolismo , Fármacos Dermatológicos/química , Composição de Medicamentos , Humanos , Mediadores da Inflamação/metabolismo , Nanomedicina , Psoríase/diagnóstico , Psoríase/imunologia , Psoríase/metabolismo , Transdução de Sinais , Pele/imunologia , Pele/metabolismo , Pele/patologiaRESUMO
The role of mushroom polysaccharides and probiotics as pharmaceutical excipients for development of nanocarriers has never been explored. In the present study an attempt has been made to explore Ganoderma lucidum extract powder (GLEP) containing polysaccharides and probiotics to convert liquid self nanoemulsifying drug delivery system (SNEDDS) into solid free flowing powder. Two lipophilic drugs, curcumin and quercetin were used in this study due to their dissolution rate limited oral bioavailability and poor permeability. These were loaded into liquid SNEDDS by dissolving them into isotropic mixture of Labrafill M1944CS, Capmul MCM, Tween-80 and Transcutol P. The liquid SNEDDS were solidified using probiotics and mushroom polysaccharides as carriers and Aerosil-200 as coating agent. The solidification was carried out using spray drying process. The process and formulation variables for spray drying process of liquid SNEDDS were optimized using Box Behnken Design to attain required powder properties. The release of both drugs from the optimized spray dried (SD) formulation was found to be more than 90%, whereas, it was less than 20% for unprocessed drugs. The results of DSC, PXRD and SEM, showed that the developed L-SNEDDS preconcentrate was successfully loaded onto the porous surface of probiotics, mushroom polysaccharides and Aerosil-200.
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Agaricales/química , Curcumina/farmacologia , Sistemas de Liberação de Medicamentos , Emulsões/química , Nanopartículas/química , Polissacarídeos/química , Probióticos/química , Quercetina/farmacologia , Análise de Variância , Células CACO-2 , Varredura Diferencial de Calorimetria , Portadores de Fármacos/química , Composição de Medicamentos , Humanos , Nanopartículas/ultraestrutura , Permeabilidade , Difração de Raios XRESUMO
Introduction: Diabetic retinopathy (DR) is associated with damage to the retinal blood vessels that lead eventually to vision loss. The existing treatments of DR are invasive, expensive, and cumbersome. To overcome challenges associated with existing therapies, various intraocular sustained release and novel drug delivery systems (NDDS) have been explored.Areas covered: The review discusses recently developed intraocular devices for sustained release of drugs as well as novel noninvasive drug delivery systems that have met a varying degree of success in local delivery of drugs to retinal circulation.Expert opinion: The intraocular devices have got very good success in providing sustained release of drugs in patients. The development of NDDS and their application through the ocular route has certainly provided an edge to treat DR over existing therapies such as anti-VEGF administration but their success rate is quite low. Moreover, most of them have proved to be effective only in animal models. In addition, the extent of targeting the drug to the retina still remains variable and unpredictable. The toxicity aspect of the NDDS has generally been neglected. In order to have successful commercialization of nanotechnology-based innovations well-designed clinical research studies need to be conducted to evaluate their clinical superiority over that of the existing formulations.
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Diabetes Mellitus , Retinopatia Diabética , Animais , Retinopatia Diabética/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Humanos , Nanotecnologia , RetinaRESUMO
BACKGROUND: Diabetic foot ulcer (DFU) is one of the leading complications of type-2 diabetes mellitus. It is associated with neuropathy and peripheral arterial disease of the lower limb in patients with diabetes. There are four stages of wound healing, namely hemostasis phase, inflammatory phase, proliferative phase and maturation phase. In the case of DFU, all these stages are disturbed which lead to delay in healing and consequently to lower limb amputation. Conventional dosage forms like tablets, creams, ointments, gels and capsules have been used for the treatment of diabetic foot ulcer for many years. INTRODUCTION: In this review, the global prevalence as well as etiopathogenesis related to diabetic foot ulcer have been discussed. The potential role of various synthetic and herbal drugs, as well as their conventional dosage forms in the effective management of DFU have been discussed in detail. METHODS: Structured search of bibliographic databases from previously published peer-reviewed research papers was explored and data has been represented in terms of various approaches that are used for the treatment of DFU. RESULTS: About 148 papers, including both research and review articles, were included in this review to produce a comprehensive as well as a readily understandable article. A series of herbal and synthetic drugs have been discussed along with their current status of treatment in terms of dose and mechanism of action. CONCLUSION: DFU has become one of the most common complications in patients having diabetes for more than ten years. Hence, understanding the root cause and its successful treatment is a big challenge because it depends upon multiple factors such as the judicious selection of drugs as well as proper control of blood sugar level. Most of the drugs that have been used so far either belong to the category of antibiotics, antihyperglycaemic or they have been repositioned. In clinical practice, much focus has been given to dressings that have been used to cover the ulcer. The complete treatment of DFU is still a farfetched dream to be achieved and it is expected that combination therapy of herbal and synthetic drugs with multiple treatment pathways could be able to offer better management of DFU.
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Diabetes Mellitus Tipo 2 , Pé Diabético , Amputação Cirúrgica , Diabetes Mellitus Tipo 2/complicações , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/epidemiologia , Pé Diabético/tratamento farmacológico , Pé Diabético/epidemiologia , Humanos , Hipoglicemiantes/uso terapêutico , CicatrizaçãoRESUMO
Introduction: Diabetic neuropathy (DN) is one of the major complications arising from hyperglycaemia in diabetic patients. In recent years polyphenols present in plants have gained attention to treat DN. The main advantages associated with them are their action via different molecular pathways to manage DN and their safety. However, they failed to gain clinical attention due to challenges associated with their formulation development such as lipophilicity,poor bioavailability, rapid systemic elimination, and enzymatic degradation.Area covered: This article includes different polyphenols that have shown their potential against DN in preclinical studies and the research carried out towards development of their nanoformulations in order to overcome aforementioned issues.Expert opinion: In this review various polyphenol based nanoformulations such as nanospheres, self-nanoemulsifying drug delivery systems, niosomes, electrospun nanofibers, metallic nanoparticles explored exclusively to treat DN are discussed. However, the literature available related to polyphenol based nanoformulations to treat DN is limited. Moreover, these experiments are limited to preclinical studies. Hence, more focus is required towards development of nanoformulations using simple and single step process as well as inexpensive and non-toxic excipients so that a stable, scalable, reproducible and non-toxic formulation could be achieved and clinical trials could be initiated.