Objective: The aim of the present study was to design novel drug delivery system containing ramipril microemulsion. Ramipril is an antihypertensive drug having very low aqueous solubility and bioavailability. Ramipril microemulsion could be used as a possible alternative to the traditional oral formulation to improve dissolution rate and hence its bioavailability with avoidance of the first-pass metabolism.Methods: The microemulsion existence region was determined by constructing pseudoternary phase diagram and prepared by using four components orange oil, tween 80 as a surfactant, propylene glycol as co-surfactant and distilled water as the aqueous phase. The water titration method was employed for its determination. All formulated microemulsion were subjected for visual inspection, centrifugation and stability test. The all stable formulations were selected for further study.The optimized microemulsion formulation B-9 was subjected for various evaluation parameters such as, visual inspection, stability studies, pH, viscosity measurements, electrical conductivity, content uniformity and dye solubility test.Results: Results revealed that construction of phase diagram and use of phase titration method was a suitable technique for the preparation of microemulsion as most of the formulations were transparent. It was found that the best microemulsion result was found for ratio 2:1. The results of stress tests conclude that the optimized formulation was both physically and chemically stable for 8 mo. Also, The Fourier transform infrared (FTIR) radiation measurement and Differential scanning calorimetry (DSC) of optimized formulation indicate the compatibility of ramipril with orange oil, surfactant-tween 80 and cosurfactant-propylene glycol. From electrical conductivity 0.283 σ and staining test the prepared optimized formulation B-9 was found to be o/w type of microemulsion. The optimized B-9 formulation showed good viscosity 13.52±0.01cps and pH 3.21±0.02 with highest drug content uniformity was found to be 84.98±0.02 %.Conclusion: In the present study a satisfactory attempt was made to formulate a novel o/w microemulsion of ramipril which improves the gastrointestinal absorption by raising its water solubility and hence oral bioavailability is also enhanced.
Objective: The purpose of present study aims to design novel drug delivery system containing oxiconazole nitrate microsponges and to prepare microsponge gel. Oxiconazole nitrate is an antifungal drug used in the treatment of fungal infection having a poor aqueous solubility, side effects and adverse reactions. The microsponge delivery system is unique technology for controlled release of active agents. Methods:The microsponges were prepared by quasi-emulsion solvent diffusion method by using polymer eudragit S-100 and eudragit L-100. All the formulated microsponges were subjected for various evaluation parameters such as production yield, encapsulation efficiency, particle size analysis and in vitro drug release study. The optimised microsponge formulation F3 and F9 were further formulated as gel formulation for topical delivery. Prepared gel was evaluated for physical parameters like pH, spreadability, viscosity, drug content and in vitro diffusion study and compared with the marketed formulation. Results:The Fourier transform infrared radiation measurement (FTIR) and Differential scanning colorimetry (DSC) of drug and excipient confirm compatibility. Results revealed that quasi-emulsion solvent diffusion method is a suitable technique for the preparation of microsponges as most of the formulations were discrete and spherical in shape with a good production yield of 61.44% to 80.45% and The highest drug release for F3 and F9 formulation was found to be 87.77 % and 83.24 % respectively for the 8 h. The microsponge gel formulation MGI (F3) showed the controlled release of oxiconazole nitrate for 12 h. The drug release data of optimised batch MGI (F3) were fitted into different kinetic models and showed that the drug release from gel formulation follows zero order release. Conclusion:As compared to conventional formulation, the prepared microsponge gel are expected to remain on the skin for a longer time, gradually releasing their contents over the time. Hence, oxiconazole nitrate microsponges and microsponge gel prepared in this study are promising as being more useful than conventional formulation therapy.
Cancer is the most ruinous disease globally. Natural products have impressive characteristics, such as excep-tional chemical versatility, chemical and biological properties of macromolecular specificity and less toxicity which make them good leads in finding novel drugs. The phytochemicals not only help to prevent but also treat chronic cancerous conditions. The present review attempts to put forth some selected anticancer phytochemicals that had reported omics char-acteristic and specifically suppressed cancer with in vitro and in vivo activity. Certain issues pertaining to anticancer phy-tochemicals like delivery to target site in the body and achieving controlled release in order to prevent overdoses havelong been a concern for medical researchers worldwide. The most conventional chemotherapy protocols for the treatment of cancer lead to adverse effects that limit biological efficacy and compromise patient outcomes. In order to defeat incompe-tency of current and upcoming natural anticancer agents and to attain targeted drug delivery with good efficacy and fewer side effects, there is a special focus on novel nanostructured particles and nano approaches consisting of carrier system. Recent studies have led to the discovery of mesoporous and nanoporous drug delivery mechanisms, such as inorganic or organic-based nanosponges. The metal based inorganic systems have exhibited toxicity and non-biodegradable character in vivo. As a result of problems related to inorganic systems, major shift of research from inorganic to organic nanosystems has occurred. About decades ago, researchers have developed organic nanosponges to control the limitation of drug delivery and cancer therapies. This review article discusses the development and application of nanosponges encapsulated phyto-chemicals for cancer therapy.
: Mannich bases identified by Professor Carl Mannich have been the most extensively explored scaffolds for more than 100 years now. The versatile biological roles that they play have promoted their applications in many clinical conditions. The present review highlights the application of Mannich bases as cytotoxic agents, categorizing them into synthetic, semisynthetic and prodrugs classes and gives an exhaustive account of the work reported in the last two decades. The methods of synthesis of these cytotoxic agents, their anti-cancer potential in various cell lines and promising leads for future drug development have also been discussed. Structure-activity relationships along with the targets on which these cytotoxic Mannich bases act have been included as well.
Background: Urbanization has commanded numerous health tribulations globally and cancer is most devastating among them. Phytochemicals have been utilized as bioactive compounds/nutrients prominently as antioxidants, revitalizing agents and found to have notable health benefits. Objectives: The nutritional constituents of plants have intensively been investigated to appraise their possessions on healthiness and effectiveness in cancer. The food supplement viz. nutraceutical has an important role in health and provides essential molecules required for different metabolic processes which regulated body functions assisting in protection of body from diseases. Methods: Numerous attempts and substantial studies have been escalated by many researchers. These studies have explained that dietary patterns and restrictions are the most important cardinal stride and determinant of many dreadful diseases like cancer. This review article focuses on the exploration of clinical significance of phytochemicals in cancer therapy Results: The phytochemicals from various plant parts having potential to prevent cancer as well as serve as effective anti-cancer agents have been summarized in terms of their components such as carotenoids, flavonoids, alkaloids, organosulphur compounds etc., along with the targets on which they act, sources from where they can be obtained and their screening procedure. The significant interest has been received in nutraceuticals because of nutritional benefits, safety and preventive as well as therapeutic perspectives. Conclusions: Phytonutraceuticals as current drug delivery for cancer have been utilized as an option for modern medicines. Ultimately, they ensure improvement in health and this review focuses an overview of current nutraceuticals and nano based delivery system which may be helpful in focusing on further groundbreaking research plans in the new domain.
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