Chitosan modified 5-fluorouracil nanostructured lipid carriers for treatment of diabetic retinopathy in rats: A new dimension to an anticancer drug.

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.

Multifaceted role of synbiotics as nutraceuticals, therapeutics and carrier for drug delivery.

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.

Chewable Tablets of Acacia catechu Extract, an Alternative to Betel (Paan) for Mouth Ulcers: Formulation and In vitro Evaluation.

OBJECTIVE: The objective of the current research work was to prepare chewable tablets having Acacia catechu extract useful for mouth ulcers using a 32 factorial design. METHODS: Acacia catechu heartwood extract was prepared using a reported method with some modifications. The extract was characterized using TLC against the catechin marker. Then, drug-excipient interaction studies were carried out. The mixture of drug and excipients was evaluated for pre-compression parameters. With the application of 32 factorial design, chewable tablets were prepared using direct compression technique. Prepared tablets were evaluated for post-compression parameters. RESULTS: In vitro drug release study of the developed formulations was investigated both in intact and crushed form of tablets. Based on the in vitro performance, the best formulations were selected (F6, F7 & F8 from intact and F1, F5 & F9 from the crushed group) and subjected to various kinetic models and evaluated for Chewing Difficulty Index (CDI). CONCLUSION: The overall results revealed that the formulated chewable tablets complied with the standards and exhibited the satisfactory performance in terms of drug release, chewing difficulty index and other related parameters.

Recent advances in intraocular and novel drug delivery systems for the treatment of diabetic retinopathy.

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.

Treatment Strategies Against Psoriasis: Principle, Perspectives and Practices.

BACKGROUND: Psoriasis is a genetically predisposed autoimmune disease mediated by cytokines released by the activated immune cells. It manifests inflammatory, scaly red or white silvery flaky skin which may be a fluid-filled lesion with soreness and itchiness. The prevalence rate of psoriasis is increasing day by day. Despite having such a high prevalence rate, the treatment of psoriasis is still limited. Hence, there is a need to rethink the various treatment strategies available in the allopathic as well as in the alternative systems of medicine. METHODS: Various bibliographic databases of previously published peer-reviewed research papers were explored and systematic data culminated in terms of various treatment strategies used for the management of psoriasis. The prime focus is given towards modern as well as alternative systems of medicine such as phototherapy, a combination of phototherapy with pharmacotherapy such as Ayurveda, Yoga and naturopathy, Unani, Siddha, and Homeopathy to treat psoriasis. RESULTS: A comprehensive review of 161 papers, including both research and review articles, was carried out to make the article readily understandable. The pathogenesis including inflammatory mediators and type of psoriasis is discussed before the treatment strategies to understand the pathophysiology of the disease. The uniqueness, procedure, advantages, and limitations of conventional, advanced, and traditional systems of medicine to treat psoriasis are discussed in detail. Emphasis has also been given towards marine sources such as fish oil, marine sponges, and algae. CONCLUSION: Although there are many modern and alternative treatment strategies available to treat psoriasis, none of them have been proven to provide complete relief to patients. Moreover, they are associated with certain side effects. In order to overcome them, novel drug delivery systems have been utilized and found effective; however, their stability and safety become the major impediments towards their successful positioning. Traditional and alternative treatment strategies have found to be safe and effective but their use is localized to certain areas. In a nutshell, to achieve successful treatment of psoriasis, there is a need to focus on the development of stable and non-toxic novel drug delivery systems or the promotion of traditional systems to treat psoriasis.

Solidification of liquid Modified Apple Polysaccharide by its adsorption on solid porous carriers through spray drying and evaluation of its potential as binding agent for tablets.

In the present study application of Modified Apple Polysaccharide (MAP) as tablet binder was evaluated. Liquid MAP was extracted from apple and solidified by adsorbing it on porous surface of Aerosil-200 and trehalose and this dispersion was dried using spray dryer. The concentration of excipients as well as spray drying conditions was optimised by using Box Behnken Design to achieve desirable powder characteristics. The optimised batch of solid MAP was characterized by DSC, PXRD, SEM, and FT-IR studies that confirmed complete adsorption of liquid MAP on the surface of Aerosil-200 and trehalose. This solid MAP was investigated for its binding efficacy for tablet formulation and its binding potential was compared with acacia and polyvinyl pyrrolidone K-30. Mesalamine (model drug) granules containing different concentration of binders were prepared by wet granulation. The granules were evaluated for micromeritic properties and results were found within the pharmacopoeial limits. The prepared tablets were subjected for post compression studies such as hardness, friability, disintegration, dissolution, physical stability, content uniformity and percentage elastic recovery and their results were found good. At 2.5% w/w concentration in tablet, the solid MAP has shown shorter disintegration time and faster dissolution profile as compared to other concentrations used including good physico-mechanical properties.