: Cancer is one of the most complicated and prevalent diseases in the world, and its incidence is growing worldwide. Natural products containing pharmacological activity are widely used in the pharmaceutical industry, especially in anticancer drugs, due to their diverse structures and distinctive functional groups that inspire new drug results by means of synthetic chemistry. Terrestrial medicinal plants have traditionally been the primary source for developing natural products (NPs). However, over the past thirty years, marine organisms such as invertebrates, plants, algae, and bacteria have revealed many new pharmaceutical compounds known as marine NPs. This field constantly evolves as a discipline in molecular targeted drug discovery, incorporating advanced screening tools that have revolutionised and become integral to modern antitumor research. This review discusses recent studies on new natural anticancer alkaloids obtained from marine organisms. The paper illustrates the structure and origin of marine alkaloids and demonstrates the cytotoxic action of new alkaloids from several structural families and their synthetic analogs. The most recent findings about the potential or development of some of them as novel medications, together with the status of our understanding of their current mechanisms of action, are also compiled.

Liposomes (LPs) are capable of transporting a wide range of bioactive compounds (BACs) that have significant applications in the pharmaceutical, food, and cosmetic industries. These BACs can be administered through various routes, including parenteral (injection), oral ingestion, or transdermal absorption. In addition, there have been limited studies conducted on the toxicological and safety aspects of LPs. This highlights the need for more research to be conducted on the potential risks of oral exposure before considering their use in food applications. Therefore, the purpose of this review is to present the latest information on the composition of LP, the materials used to coat LPs for applications in the pharmaceutical and food industries to enhance the stability of LPs containing delicate BACs, and the absorption of LPs and commercially available liposomal products produced using different technologies in the market. In addition, this paper revisits various advanced technologies used in the field of food and nutraceutical processing. These technologies include the supercritical fluid method, supercritical antisolvent method, supercritical reverse phase evaporation method, micro-fluidization, and ultrasonication. The article also discusses the applications of these technologies.

Endophthalmitis, an inflammatory condition of the intraocular cavity, poses a significant challenge in ophthalmology due to its rapid progression and potential for vision loss. Conventional treatment modalities, such as systemic antibiotics or oral administration, often face limitations in achieving the required therapeutic levels at the target site. Hence, repeated intravitreal injections of antibiotics are currently the most preferred and recommended therapy for the management of endophthalmitis, which is an invasive technique and has certain shortcomings, elevated intraocular pressure, bleeding inside the eye, heightened likelihood of retinal detachment, retinal toxicity, and many more. Vancomycin is the first choice drug for the management of endophthalmitis and is given through intravitreal injection. The work aims to design, develop, and evaluate Vancomycin-loaded NLCs incorporated into an in-situ gel offering a new non-invasive therapeutic option for the management of Endophthalmitis. The Vancomycin-loaded NLCs were successfully produced through a double emulsion/ solvent evaporation method employing a Box Behnken design. The optimized formulations were incorporated into an in-situ gel system by varying the concentration of Pluronic F127. The formulated gels were characterized for several parameters such as physical appearance, pH, viscosity, gelling strength, gelation temperature, in vitro release profile, and ex-vivo permeation study. The result revealed that the formulation had a smooth appearance with a pH range from 7 to 7.5, was near the physiological pH of the eye, had content in the range of 97.5 ± 1.0 %to 99.2 ± 1.0 % and gelation temperature near body temperature. The data of release study formulation (VISG2) revealed sustained drug release compared to the control gel. The data ex vivo permeation study revealed that there was approximately a 3 folds increase in permeation of drug form (VISG2) compared to control gel (p˂0.0001) and significant (2.02folds) permeation compared to commercially available formulation (p˂0.0001). In conclusion, the Vancomycin-loaded NLCs incorporated in-situ gel may serve as a feasible alternative to invasive intravitreal injection for the management of endophthalmitis.

Hydrophilic drugs are proficient therapeutic drug candidates; however, their effective delivery poses a formidable challenge. Therefore, the development of an efficient drug delivery system demands a multifaceted approach. In recent decades, nanolipid carriers have emerged as promising drug delivery systems, offering enhanced stability, improved bioavailability, and controlled release profiles. Although nanolipid carriers have been widely investigated as carriers for hydrophobic drugs and have demonstrated remarkable success in encapsulating hydrophobic drugs, encapsulating a hydrophilic drug moiety still remains a challenge.The current study provides a comprehensive review of innovative methods developed for the successful encapsulation of hydrophilic drugs into nanolipid carriers. The first section of the study explores the physicochemical properties of hydrophilic drugs and the inherent challenges associated with their encapsulation in lipid-based carriers. The subsequent sections delve into the various strategies employed to overcome these challenges. Emphasis is placed on novel formulation techniques investigated for the encapsulation of hydrophilic drugs into nano lipid carriers. The present review not only delineates the various traditional methods for high entrapment of hydrophilic drugs but also underscores modifications to the hydrophilic drug candidates, facilitating their efficient encapsulation into nanolipid carrier drug carriers.This study explores the current state of knowledge regarding methods for encapsulating hydrophilic drugs into nanolipid carriers. By addressing the challenges associated with hydrophilic drug encapsulation and presenting innovative strategies, this review aims to provide valuable insights to researchers and pharmaceutical scientists working in the field of nanomedicine and drug delivery.

: Dermatological disease states have psychological impacts that affect a patient’s life. In the management of such disorders, topical delivery has an important role. However, the conven-tional topical delivery systems suffer from various limitations, like skin irritation, a minute quan-tity of drugs reaching disease sites, and over and under medication, which leads to an adverse re-action and therapeutic failure, respectively. Therefore, researchers continuously search for an al-ternate delivery system for treating skin disease. In recent years, nanostructured lipid carriers (NLC) have emanated as promising carrier systems for topical delivery. The current review pro-vides an in-depth insight into topical administration for treating a variety of dermatological issues using NLCs as a carrier. This review highlights the suitability of NLCs as carriers for topical de-livery, their method of preparation, and their characterization. In the present review, the main emphasis has been given to the management of various dermatological problems by using NLCs as a carrier; a plethora of literature investigating NLC as the carrier for topical delivery has been included in this review. In this paper, an attempt has been made to provide a summary of the re-search carried out in this field that will encourage further research in this arena.

BACKGROUND:The disease of the posterior segment of the eye is a major concern worldwide, and it affects more than 300 million people and leads to serious visual deterioration. The current treatment available is invasive and leads to serious eye complications. These shortcomings and patient discomfort lead to poor patient compliance. In the last decade, Nanostructured lipid carriers (NLC) have established a remarkable milestone in the delivery of drug substances to the posterior segment of the eye. Additionally, NLC can reduce the clearance due to adhesive properties which are imparted due to nano-metric size. This attribute might reduce the adverse effects associated with intravitreal therapy and thus enhance therapeutic efficacy, eventually raising patient adherence to therapy. The current review provides an inclusive account of NLC as a carrier to target diseases of the posterior segment of the eye.OBJECTIVE:The review focuses on the various barrier encountered in the delivery of drugs to the posterior segment of the eye and the detail about the physicochemical property of drug substances that are considered to be suitable candidates for encapsulation to lipid carriers. Therefore, a plethora of literature has been included in this review. The review is an attempt to describe methods adopted for assessing the in-vivo behavior that strengthens the potential of NLC to treat the disease of the posterior segment of the eye.CONCLUSION:These NLC-based systems have proven to be a promising alternative in place of invasive intravitreal injections with improved patient compliance.

There is a connection between bioavailability and absorption. In the field of pharmacology, this is referred to as a category of absorption and is defined as the proportion of a particular dosage of a drug that does not change and is absorbed into the systemic circulation. Both the overall absorption of medications and their specific bioavailability are important factors to consider in treatment. In this paper, we will go into great detail about the bioavailability of phytochemicals. We will also discuss the factors that influence bioavailability, the processes that improve bioavailability, and the phytochemicals that act as important bio enhancers, which are agents that improve the bioavailability of drugs.

Background: Delivery of anti-cancer agents is challenging due to some inherent problems associated with them like instability, low solubility, non-specificity, variable pharmacokinetics, narrow therapeutic window, multi-drug resistance development, and other physiological barrier related to tumor cells. In recent years, Nanostructured lipid carrier (NLC) has gained considerable importance in improving anti-cancer agents' therapeutic efficacy. Objective: The present review furnishes a comprehensive account of various barriers encountered in delivering the anti-cancer agent, the suitability of NLC to deliver anti-cancer agent, the techniques employed for the fabrication of NLC, its structure, along with its characterization. The main emphasis has given a break worth to overcome barriers in delivering chemotherapeutic through NLC so far; a number of qualitative literature have been included in this review. Further, the study describes the stability issue associated with the long-term storage of NLC. Conclusion: The NLCs systems offer a great potential to target various anti-cancer agents suffering from low solubility, non-specificity, and severe adverse effects. The NLC system's development can overcome barriers encountered in delivering anti-cancer agents and improve its efficacy in various melanoma types.

Solid lipid nanoparticles (SLN) encapsulating miconazole nitrate (MCN), with topical administration purposes for effective treatment of fungal skin infections, were formulated by a method that avoids the use of sonication or organic solvents. To facilitate the controlled release and skin targeting potential, the optimized SLN were incorporated into Carbopol hydrogels and characterized for physical appearance, homogeneity, drug content, pH, viscosity, spreadability and in vitro drug release. Based on the above parameters, H-SLN2 formulation containing 0.5% w/w Carbopol 934 was selected as optimized hydrogel formulation. The H-SLN2 formulation was compared with corresponding marketed gel product for in vitro drug release studies, ex vivo skin permeation and retention studies, skin irritation studies and in vivo antifungal activity. Drug release from H-SLN2 followed Korsmeyer-Peppas model with anomalous non-Fickian release mechanism. The skin retention studies across the rat skin revealed 1.63-fold greater retention of MCN in stratum corneum and 1.56-fold more accumulation of MCN in skin, in the case of H-SLN2 compared to marketed product. The in vivo antifungal studies confirmed the higher therapeutic efficacy of H-SLN2 against Candida albicans in comparison to marketed product. The H-SLN2 exhibited physicochemical stability at 5 °C ± 3 °C and 25 °C ± 2 °C/60% RH ± 5% RH up to 6 months. It was concluded that SLN containing Carbopol hydrogel had good skin targeting ability in conjunction with sustained release and drug localized effect, and it may serve as potential carrier for topical delivery of MCN in the effective treatment of cutaneous mycoses.

In the present study, an attempt was made to fabricate Miconazole nitrate (MCN)-loaded solid lipid nanoparticles (SLN) by hot high shear homogenization method (HSHM).Box-Behnken design (BBD) was employed as an experimental design to optimize the formulations consisting of three levels, four factors, and three center points.The design matrix of BBD consisted of 27 runs by employing 5 responses, i.e., average particle size, polydispersity index, zeta potential, percent encapsulation efficiency, and percent drug loading.The four factors selected were drug:tristearin (% w/w), Tween 80 (% w/v), homogenization speed (rpm), and homogenization time (minutes).Contour plots and 3D response surface plots were generated.The MCN-loaded optimized SLN formulation was prepared by setting the formulation factors of hot HSHM according to the solution given by BBD at a drug:tristearin ratio of 7.3727 (%w/w), Tween 80 concentration of 15% (w/v), homogenization speed of 17,000 rpm, and homogenization time of 20 minutes.The optimized formulation was subjected to differential scanning calorimetry, Fourier transform infrared spectroscopy, and field emission scanning electron microscopy study.In vitro drug release kinetic study of optimized formulation followed the Korsmeyer-Peppas model (regression coefficient value of 0.945) and it was found to be stable for 6 months at 5°C ± 3°C.These results reveal the successful development of MCN-loaded SLN by hot HSHM.

Objective: The main objective of this study was to develop and evaluate the eudragit and HPMC coated metformin hydrochloride floating microspheres, in which HPMC helps in floating and eudragit as a coating material for a site-specific drug release in a controlled manner and the active moiety metformin used as anti-hyperglycemic agent. Methods: The floating microsphere was prepared by the solvent evaporation method incorporating metformin as a model drug. The prepared floating microsphere were characterized for particle size, %yield, drug loading and entrapment efficiency, compatibility study, %buoyancy, surface morphology and In vitro drug release and release kinetics. Results: The result metformin loaded floating microsphere was successfully prepared and the particle size range from 397±23.22 to 595±15.82 µm, the entrapment efficiency range from 83.49±1.33 to 60.02±1.65% and drug loading capacity range from 14.3±0.54 to 13.31±0.47% and %buoyancy range from 85.67±0.58 to 80.67±1.15%. The FT-IR and X-RD analysis confirmed that no any interaction between drug and excipient, and surface morphology confirmed those particles are sphere. The floating microsphere show maximum 96% drug release in pH 0.1N HCL and follow the Korsmeyer peppas model of the super case-2 transport mechanism. Conclusion: These results suggest that metformin loaded floating microspheres could be retain in stomach for long time and give site specific drug release in controlled manner.

Beta-Cyfluthrin is one of the most widely used type-II pyrethroid in agriculture.Toxic effects of beta-cyfluthrin are due to the presence of cyano moiety in its chemical structure.This study was designed the effect of betacyfluthrin at different doses on brain tissue, the most important vital organ in animal body and in which dose level beta-cyfluthrin shows its effects.Animal were initially divided into control and beta-cyfluthrin given groups.There were five animals in the control group and twenty five animals in beta-cyfluthrin administered group.The latter was divided into five equal subgroups: 35.48, and 5.06, 2.53, 1.68, 1.27mg/kg body weight of beta-cyfluthrin administered groups, acute (1 day) and sub-acute (7, 14, 21 and 28 days) by gavage respectively.Control group was given only water.The effect of these treatments were studied on activities of four potential biomarkers were assayed in the brain of albino rat along with neurosomatic index viz.Body weight, brain weight and brain weight body weight ratio and neurobehavioural changes.Beta-cyfluthrin treatment resulted in a significant decrease in brain acetyl-cholinesterase.Acetylcholinesterase which found to be decreased (inhibition range 53 to 18%) in albino rats after acute and sub-acute treatment (vide-supra).Further glutathione-s-transferase (GST) was also found to be decreased in brain of albino rats (inhibition range 47 to29%) after beta-cyfluthrin administration.Again brain adenosine triphosphtase (total ATPase) activity was seen to decrease in albino rats (inhibition range 36 to19%) along with succinic dehydrogenase (SDH) was also seen decreased in brain of albino rats (inhibition range 31 to 9%)) after acute and sub-acute beta-cyfluthrin intoxication.Further hypnoatremia (inhibition range 31 to 20%) along with hypokalemia (inhibition range 19 to 14%) has also been observed after acute and sub-acute intoxication of beta-cyfluthrin.Apart from AChE, which is a specific marker of pyrethroid neurotoxicity, the levels of brain GST, ATPase, SDH along with Na and K may serve as important determinants of beta-cyfluthrin induced neuronal dysfunctioning along with neurobehavioural alterations; outcomes of fluctuated brain biochemistry because clinical signs of toxicity were observed in animals which received different doses of beta-cyfluthrin after 7 th , and 14 th days of sub-acute treatment.Animals showed overt cholinergic signs which included salivation, excitability, ataxia, muscle twisting, followed by general tremors and lethargyness.The treated groups did not reveal any mortality.Exposure of animals to beta-cyfluthrin caused extensive changes in neurosomatic, neurochemical and neurobehavioural parameters.So, oral administration of beta-cyfluthrin leads to negative response on animal health.

The transdermal route of administration has been recognized as one of the highly potential routes. Transdermal drug delivery systems deliver the drugs across epidermis to achieve systemic effects and also it control, the delivery of drugs by employing an appropriate polymer. The objective of the present work was to develop a suitable transdermal drug delivery system of Gatifloxacin. Gatifloxacin is a fourth generation quinolone and used in the treatment of bacterial infections like bronchitis typhoid tuberculosis urinary tract disease etc. Polymeric films of Gatifloxacin were prepared by the solvent evaporation technique on mercury substrate. The physicochemical compatibility of the drug and the polymers were studied by infrared spectroscopic and studies. Transdermal patches were prepared with different ratios of combination of polymers like ERS100: ERL100, ERL100: EC. They were evaluated for physicochemical parameter in vitro release and ex vivo permeation. Release of the drug from the films followed anomalous transport (0.5 < n <1). Polymeric combination containing in ratio (ERS100: ERL: 2:1) (F 2) was considered as the best formulation with maximum drug release of 92% after 12 hrs. The flux of formulation F2 was found to be greater than the other formulations.

This study was aimed to statistically optimize CODES (TM) based Piroxicam (PXM) tablet for colon targeting. A 3 2 full factorial design was used for preparation of core tablet that was subsequently coated to get CODES (TM) based tablet. The experimental design of core tablets comprised of two independent variables: amount of lactulose and PEG 6000, each at three different levels and the dependent variable was %CDR at 12 h. The core tablets were evaluated for pharmacopoeial and non-pharmacopoeial test and coated with optimized levels of Eudragit E100 followed by HPMC K15 and finally with Eudragit S100. The in vitro drug release study of F1-F9 was carried out by change over media method (0.1 N HCl buffer, pH 1.2, phosphate buffer, pH 7.4 and phosphate buffer, pH 6.8 with enzyme b-galactosidase 120 IU) to select optimized formulation F9 that was subjected to in vivo roentgenography. Roentgenography study corroborated the in vitro performance, thus providing the proof of concept. The experimental design was validated by extra check point formulation and Diffuse Reflectance Spectroscopy revealed absence of any interaction between drug and formulation excipients. The shelf life of F9 was deduced as 12 months. Conclusively, colon targeted CODES (TM) technology based PXM tablets were successfully optimized and its potential of colon targeting was validated by roentgenography.

The aim of the study was to reveal the neurotoxic effect of an orally administered beta-cyfluthrin, a type-II pyrethroid in albino rats on the basis of activity of brain GST (Glutathione-s-transferase), AChE (acetylcholinesterase) and of total proteins level at different doses 35.48 and 5.06, 2.53, 1.68, 1.27 mg/kg body weight, for acute (1 day) and sub-acute (7, 14, 21 and 28 days) treatments respectively. Results reveal that beta-cyfluthrin administration inhibits AChE activity and GST activity, however, no significant effect in total brain proteins could be observed. Affinity towards the hydrophobicity of xenobiotic substance (experimental compound) may lead to an inhibitory mechanism of both AChE and GST levels. Further, imbalance in the neurotransmitter level and alterations in the detoxification mechanism in brain is suggestive of additional mode of action of beta-cyfluthrin other than AChE inhibition. Keywords: Glutathione-s-transferase (GST), acetylcholinesterase (AChE), beta-cyfluthrin, detoxification, albino rats