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1.
Heliyon ; 10(8): e29429, 2024 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-38628770

RESUMO

Polyelectrolyte complexes (PECs) formed by the interaction between oppositely charged polymers have emerged as promising carriers for accomplishing colon-specific release. In this study, we have explored the potential of polyelectrolyte complexes between a succinate derivative of Leucaena leucocephala galactomannan and cationic guar gum for colon delivery of synbiotic. The PECs were prepared using a polyelectrolyte complexation method and characterized. The PECs exhibited excellent stability, with high encapsulation efficiency for both probiotics (95.53 %) and prebiotics (83.33 %). In vitro studies demonstrated enhanced survivability and proliferation of the encapsulated probiotics in the presence of prebiotics (93.29 %). The SEM images revealed a smooth and firm structure with reduced number of pores when both prebiotic and probiotic were encapsulated together. The treatment with synbiotic PECs in acetic acid induced IBD rats significantly relieves colitis symptoms as was evident from colon/body ratio, DAI score and histopathology studies. An increase in the protein and reduced glutathione levels and reduction in superoxide dismutase activity was observed in colitic rats that received synbiotic treatment as compared to colitic rats. Overall, this study highlights the potential of Leucaena leucocephala succinate-cationic guar gum PECs as a promising system for colon-specific synbiotic delivery, with implications for improved gut health and the treatment of various gastrointestinal disorders.

2.
Artigo em Inglês | MEDLINE | ID: mdl-38204233

RESUMO

BACKGROUND: Bacterial infections are becoming difficult to treat nowadays due to the development of resistance towards conventional treatments. Conventional topical formulations loaded with antibiotics display various disadvantages, like high dosing frequency, high toxicity, and poor patient compliance. The former limitations may sometimes lead to severe complications and hospitalization of patients. However, these can be overcome by employing vesicular nanocarriers for the delivery of antibiotics following the topical/transdermal route. OBJECTIVE: The objective of this review paper was to summarize the role of vesicular nanocarriers, like liposomes, elastic liposomes, niosomes, ethosomes, solid lipid nanoparticles, nanostructured lipid carriers, and nanoemulsions for topical/transdermal delivery of antibiotics, and patents associated with them. METHODS: Literature for the present review was collected using various search engines, like PubMed, Google Scholar, and Google Patents. RESULTS: Various literature investigations have revealed the in vitro and preclinical efficacy of vesicular nanocarrier systems in the delivery of antibiotics following the topical/transdermal route. CONCLUSION: Vesicular nanocarrier systems, via targeted delivery, may subside various side effects of antibiotics associated with conventional delivery, like high dosing frequency and poor patient compliance. However, their existence in the pharmaceutical market will be governed by effective clinical assessment and scale-up methodologies.

3.
Artigo em Inglês | MEDLINE | ID: mdl-34961431

RESUMO

BACKGROUND: Dermatological disorders are cutaneous infirmities which are frequently occurring and increasing at an alarming rate. These range from mild itching/redness (dermatitis) to fatal skin cancers and has posed a major health concern. Azadirachta indica A. Juss (commonly known as neem), a member of Meliaceae family, is an Indian medicinal plant which has been known for its health promoting effects since ancient times. OBJECTIVE: The review highlights the traditional practices, pharmacological aspects, and formulatory approach of neem for the treatment of dermatological disorders. Further, recent patents and novel delivery systems (developed and in pipeline) improving skin delivery and therapeutic profile of neem are discussed. RESULTS: Neem is a traditional medicinal plant that has been employed for the prevention and treatment of numerous ailments covering systemic and topical disorders. Scientific studies have validated the traditional claims of neem and attributed these health benefits to the presence of more than 300 structurally diverse and complex compounds. It possesses anti-inflammatory, antibacterial, analgesic, antiviral, antifungal, immunomodulatory and antioxidant activities which substantiate its use as skin therapy. Various novel formulations and associated patents that improved the permeability of neem based products across skin could be found in literature. CONCLUSION: Critical appraisal of available literature revealed that neem possesses anti-microbial, anti-inflammatory, antioxidant and antiseptic properties. Thus it has the potential to be developed as a single effective therapy for the management of multimodal skin disorders. Further, pharmaceutical tailoring of neem by implication of novel carriers could enhance its penetrability across skin.


Assuntos
Azadirachta , Plantas Medicinais , Extratos Vegetais/uso terapêutico
4.
Recent Adv Antiinfect Drug Discov ; 16(3): 196-208, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34844552

RESUMO

BACKGROUND: The prevalence and scope of dermatological illness differ from region to region. Based upon type and severity, the conditions may vary from superficial to deep systemic skin infections. Niacinamide, an amide analog of vitamin B3 which was conventionally utilized as a food supplement, is now explored for the management of skin disorders. Being a powerhouse on its own, it is not stored inside the body naturally and has to be acquired from external sources. Areas Covered: This review is an attempt to disclose the physiology, pharmacology, and highlight the dermatological potentials of niacinamide, discussing its pharmacological mechanisms, varied commercially available treatments, and novel approaches, i.e., in research and patented formulations. RESULTS: Niacinamide has been verified in treating almost every skin disorder, viz. aging, hyperpigmentation, acne, psoriasis, pruritus, dermatitis, fungal infections, epidermal melasma, non-melanoma skin cancer, etc. It has been reported to possess numerous properties, for instance, anti-inflammatory, antimicrobial, antioxidant, antipruritic, and anticancer, which makes it an ideal ingredient for varied dermal therapies. Long term use of niacinamide, regardless of the skin type, paves the way for new skin cells, making skin healthier, brighter, and hydrated. CONCLUSION: Niacinamide possesses a variety of positive characteristics in the field of dermatology. Novel approaches are warranted over current treatments which could bypass the above shortcomings and form an effective and stable system. Hence, niacinamide has the potential to become an individual and a productive component with wide future scope.


Assuntos
Acne Vulgar , Cosmecêuticos , Dermatopatias , Aptidão , Humanos , Niacinamida/uso terapêutico
5.
Curr Drug Res Rev ; 13(3): 222-229, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34042044

RESUMO

Azelaic acid (AZA) is a white crystalline dicarboxylic acid naturally found in grains, rye, and barley. AZA has substantial biological and therapeutic abilities (viz a viz) its anti-inflammatory, anti-oxidant, anti-keratinizing, anti-microbial properties, etc., which contribute to its applicability in the management of mild to harsh dermatological complications (acne, rosacea, dermatitis, hyper-pigmentation, carcinomas, etc.). AZA has shown its effectiveness against varied non-inflammatory and inflammatory lesions by normalizing hyper-keratinization state and attenuating the increased levels of microbial content. Topically AZA, either alone or in conjunction with other active moieties, has proved to effectively prevent acne and several other hyper-pigmentary conditions. Chronic applicability of AZA has been evidenced with the effects like itching, burning, stinging, redness, etc. To deal with the former issues, research is being conducted to substitute the conventional formulations with novel preparations (liposome's, niosomes, micro sponges, lipid nanocarriers, etc.), which could enhance the overall pharmaceutical and pharmacological profile of the drug. This article is an attempt to highlight the basic physiochemical properties of AZA, its physiological role (especially in dermatology), various commercial preparations and recent novel approaches that are in research with an aim to augment the therapeutic and safety profile of AZA.


Assuntos
Cosmecêuticos , Fármacos Dermatológicos , Aptidão , Fármacos Dermatológicos/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Humanos
6.
Artigo em Inglês | MEDLINE | ID: mdl-33183208

RESUMO

AIM: To formulate and preliminary evaluated polysaccharide based mucoadhesive floating tablets of Cinnarizine. BACKGROUND: Gastro-retentive drug delivery systems has proved to be a successful approach to enhance the gastric residence with site specific targeting for achieving local or generalized effect. Various patents has also been filed globally employing gastro-retentive approach. OBJECTIVE: The study is designed to explore the mucoadhesive and low density characteristics of corn fibre gum (CFG) for preparation of gastro-retentive floating tablets of cinnarizine. METHODS: Floating tablets were prepared by direct compression technique using different concentrations of CFG (45, 50, 60% w/w). The formulated floating tablet batches were evaluated for their hardness, friability, drug content, floating duration/ lag time, swelling behavior, bioadhesive strength and in vitro drug release. RESULTS: Mucoadhesive strength was found to increase with an increment in the polysaccharide concentration. Swelling index was found to increase both with the increase in CFG concentration and with duration for which tablet remains in medium. The in vitro drug release studies indicated decrease in drug release (91% to 77%) with the increase in polymer concentration. The release data was further fitted to various kinetic models which revealed the drug release to be in accordance with Zero-order and Higuchi models, indicating polymer to exhibit the swellable matrix forming abilities. The value of n (between 0.458 and 0.997) from Korsemeyer Peppas model depicted the possibility of drug to follow more than one mechanism of release from the formulation i.e. diffusion and erosion. Stability studies revealed the preparations to retain their integrity and pharmaceutical characteristics at variable storage conditions. CONCLUSION: Thus from the research findings, CFG could be concluded to possess potential binder, release retardant and mucoadhesive characteristics which could be successfully employed for the formulation of gastro-retentive floating tablets.

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