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This research was designed to identify thermodynamically and kinetically stable lipidic self-emulsifying formulations through simple energy dynamics in addition to highlighting and clarifying common ambiguities in the literature in this regard. Proposing a model study, this research shows how most of the professed energetically stable systems are actually energetically unstable, subjected to indiscriminate and false characterization, leading to significant effects for their pharmaceutical applications. A self-emulsifying drug delivery system (SEDDS) was developed and then solidified (S-SEDDS) using a model drug finasteride. Physical nature of SEDDS was identified by measuring simple dynamics which showed that the developed dispersion was thermodynamically unstable. An in vivo study of albino rats showed a three-fold enhanced bioavailability of model drug with SEDDS as compared to the commercial tablets. The study concluded that measuring simple energy dynamics through inherent properties can distinguish between thermodynamically stable and unstable lipidic systems. It might lead to correct identification of a specific lipidic formulation and the application of appropriate characterization techniques accordingly. Future research strategies include improving their pharmaceutical applications and understanding the basic differences in their natures.
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The basic aim of the study was to develop and evaluate the triple drug loaded cationic nano-vesicles (cNVs), where miltefosine was used as a replacement of surfactant (apart from its anti-leishmanial role), in addition to meglumine antimoniate (MAM) and imiquimod (Imq), as a combination therapy for the topical treatment of cutaneous leishmaniasis (CL). The optimized formulation was nano-sized (86.2⯱â¯2.7â¯nm) with high entrapment efficiency (63.8⯱â¯2.1% (MAM) and 81.4⯱â¯2.3% (Imq)). In-vivo skin irritation assay showed reduced irritation potential and a decrease in the cytotoxicity of cNVs as compared to conventional NVs (having sodium deoxycholate as a surfactant). A synergistic interaction between drugs was observed against intracellular amastigotes, whereas the in-vivo antileishmanial study presented a significant reduction in the parasitic burden. The results suggested the potential of surfactant free, triple drug loaded cNVs as an efficient vehicle for the safe topical treatment of CL.
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Antiprotozoarios , Leishmania , Leishmaniasis Cutánea , Administración Tópica , Antiprotozoarios/farmacología , Humanos , Leishmaniasis Cutánea/tratamiento farmacológico , TensoactivosRESUMEN
Transdermal delivery system has gained significance in drug delivery owing to its advantages over the conventional delivery systems. However, the barriers of stratum corneum along with skin irritation are its major limitations. Various physical and chemical techniques have been employed to alleviate these impediments. Among all these, transfersomes have shown potential for overcoming the associated limitations and successfully delivering therapeutic agents into systemic circulation. These amphipathic vesicles are composed of phospholipids and edge activators. Along with providing elasticity, edge activator also affects the vesicular size and entrapment efficiency of transfersomes. The mechanism behind the enhanced permeation of transfersomes through the skin involves their deformability and osmotic gradient across the application site. Permeation enhancers can further enhance their permeability. Biocompatibility; capacity for carrying hydrophilic, lipophilic as well as high molecular weight therapeutics; deformability; lesser toxicity; enhanced permeability; and scalability along with potential for surface modification, active targeting, and controlled release render them ideal designs for efficient drug delivery. The current review provides a brief account of the discovery, advantages, composition, synthesis, comparison with other cutaneous nano-drug delivery systems, applications, and recent developments in this area.
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Portadores de Fármacos , Liposomas , Administración Cutánea , Portadores de Fármacos/metabolismo , Sistemas de Liberación de Medicamentos , Liposomas/metabolismo , Piel/metabolismo , Absorción CutáneaRESUMEN
Uncontrolled bleeding remains the leading cause of morbidity and mortality across the entire macrocosm. It refers to excessive loss of blood that occurs inside of body, due to unsuccessful platelet plug formation at the injury site. It is not only limited to the battlefield, but remains the second leading cause of death amongst the civilians, as a result of traumatic injury. Startlingly, there are no effective treatments currently available, to cater the issue of internal bleeding, even though early intervention is of utmost significance in minimizing the mortality rates associated with it. The fatal issue of uncontrolled bleeding is ineffectively being dealt with the use of pressure dressings, tourniquet, and surgical procedures. This is not a practical approach in combat arenas or in emergency situations, where the traumatic injury inflicted is deep inside the body, and cannot be addressed externally, by the application of topical dressings. This review focuses on the traditional hemostatic agents that are used to augment the process of hemostasis, such as mineral zeolites, chitosan based products, biologically active agents, anti-fibrinolytics, absorbable agents, and albumin and glutaraldehyde, as well as the micro- and nano-based hemostatic agents such as synthocytes, thromboerythrocytes, thrombosomes, and the synthetic platelets.
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Hemorragia/tratamiento farmacológico , Hemostáticos/química , Albúminas/química , Animales , Vendajes , Plaquetas/metabolismo , Celulosa/química , Quitosano/química , Colágeno/química , Glutaral/química , Hemostasis , Hemostáticos/farmacología , Humanos , Almidón/química , Zeolitas/químicaRESUMEN
The flustering rise in cancer incidence along with treatment anomalies has made cancer the second leading cause of death globally. The total annual economic impact of cancer is pronounced and is increasing. Besides the lack of proper curative therapy, treatment associated adverse effects, drug resistance, and tumor relapse are the instigations behind increased morbidity and mortality. Meanwhile, the survival rate has inclined impressively. In the last few decades, cancer treatment has undergone wide refinements aiming towards cancer prevention, complete tumor regression, subsiding treatment adverse effects, improving patient's life standard and avoiding tumor relapse. Chemotherapy has been successfully extended towards natural, cheaper and bioactive anti-inflammatory agents manifesting potent anticancer activity. Antibody-based cancer therapy has become well established as a vital and effective strategy for treating hematological malignancies as well as solid tumors. Individualized immunotherapy is becoming the forefront of cancer treatment enabling personalized, precise and patient's cancer mutanome specific adjustable regimen. The emergence of anti-neoangiogenesis and cancer stem cell targeting techniques have dropped cancer recurrence significantly. Advancements in hyperthermia and photodynamic therapies along with improvements in cancer vaccination have declined death rate and amplified survival rate convincingly.
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INTRODUCTION: Lipid-based drug delivery systems (LBDDS) are the most promising technique to formulate the poorly water soluble drugs. Nanotechnology strongly influences the therapeutic performance of hydrophobic drugs and has become an essential approach in drug delivery research. Self-nanoemulsifying drug delivery systems (SNEDDS) are a vital strategy that combines benefits of LBDDS and nanotechnology. SNEDDS are now preferred to improve the formulation of drugs with poor aqueous solubility. Areas covered: The review in its first part shortly describes the LBDDS, nanoemulsions and clarifies the ambiguity between nanoemulsions and microemulsions. In the second part, the review discusses SNEDDS and elaborates on the current developments and modifications in this area without discussing their associated preparation techniques and excipient properties. Expert opinion: SNEDDS have exhibit the potential to increase the bioavailability of poorly water soluble drugs. The stability of SNEDDS is further increased by solidification. Controlled release and supersaturation can be achieved, and are associated with increased patient compliance and improved drug loads, respectively. Presence of biodegradable ingredients and ease of large-scale manufacturing combined with a lot of 'drug-targeting opportunities' give SNEDDS a clear distinction and prominence over other solubility enhancement techniques.