Design of an Oral Tablet Containing Furosemide Nanoparticles with Elevated Bioavailability.

The solubility and permeability of the Biopharmaceutics Classification System (BCS) class IV drugs, such as furosemide (FUR), are low. Thus, the oral bioavailability of these drugs needs to be augmented. Here, we aimed to design orally disintegrating tablets containing FUR nanoparticles to improve bioavailability after oral administration.

Recovery from indomethacin-induced gastrointestinal bleeding by treatment with teprenone.

Background: Gastrointestinal injuries caused by nonsteroidal anti-inflammatory drugs (NSAIDs) is a serious side effect in patients with rheumatoid arthritis (RA). However, effective therapeutic strategies have yet to be established. In this study, we investigated the therapeutic effects of teprenone (TEP), a gastric mucosal protective drug, on NSAID-induced gastrointestinal injuries in rats with RA (AA rats).

Studies on pomegranate seed oil enriched galantamine hydrobromide microemulsion: formulation, in vitro antioxidant and neuroprotective potential.

Pomegranate seed oil with its high levels of phenolic compounds is known to exhibit neuroprotective effects. Delivering hydrophilic drugs to the brain is challenging since blood-brain barrier allows only a few lipophilic molecules into the brain, thus posing an additional barrier for drug delivery to the brain in conditions like Alzheimer's. The present study focuses on the preparation of the stable galantamine hydrobromide (GHBr) microemulsion (ME) using pomegranate seed oil (PSO) as an adjuvant.

Role of mucoadhesive agent in ocular delivery of ganciclovir microemulsion: cytotoxicity evaluation in vitro and ex vivo.

Purpose: The aim of the present study was to investigate increase in delivery of drug upon formulation as mucoadhesive microemulsion system and further to investigate possibility of any cytotoxic effects using such formulation.

Material And Methods: Considering hydrophilic and small molecular nature of the drug, it was attempted to be formulated as microemulsion, by using pseudo ternary phase diagram method. Thus, three types of microemulsions were prepared; oil in water, water in oil type and chitosan-coated microemulsion.

An understanding of mitochondria and its role in targeting nanocarriers for diagnosis and treatment of cancer.

Nanotechnology has changed the entire paradigm of drug targeting and has shown tremendous potential in the area of cancer therapy due to its specificity. In cancer, several targets have been explored which could be utilized for the better treatment of disease. Mitochondria, the so-called powerhouse of cell, portrays significant role in the survival and death of cells, and has emerged as potential target for cancer therapy.

Triamcinolone Acetonide-Loaded PEGylated Microemulsion for the Posterior Segment of Eye.

Present work investigates the possibility of a polyethyleneglycolylated (PEGylated) microemulsion (ME) to deliver drug to the posterior segment of eye. Triamcinolone acetonide (TA), a widely used drug in intraocular diseases, was selected as the model drug. Based on solubility and emulsification capacity, components of microemulsion were selected and optimum formulation was obtained using a pseudoternary phase diagram.

Comparative evaluation of fish oil and butter oil in modulating delivery of galantamine hydrobromide to brain via intranasal route: pharmacokinetic and oxidative stress studies.

The present study investigates the role of fish oil (FO)- and butter oil (BO)-enriched microemulsion-based system of galantamine hydrobromide (GH), an anti-Alzheimer drug, for its potential role in brain permeation enhancement and neuroprotection against oxidative stress. Microemulsion (ME)-based system of GH was prepared using water phase titration. The prepared ME was characterized by several physicochemical parameters like particle size, polydispersity index, and ex vivo drug permeation.

PEGylated microemulsion for dexamethasone delivery to posterior segment of eye.

Dexamethasone (Dex) is one of the most commonly used anti-vascular endothelial growth factor (anti-VEGF) drugs being used in ocular diseases whether it is associated with anterior segment or posterior segment. For diseases of posterior segment of eye, Dex is delivered as intravitreal implant but the route used for the same is very invasive and poses several hazards on long term use. Thus, topical formulation with ability to outreach retina from ocular surface was intended.

Role of Omega-3 Fatty Acids and Butter Oil in Targeting Delivery of Donepezil Hydrochloride Microemulsion to Brain via the Intranasal Route: a Comparative Study.

In order to investigate the possible role of butter oil (BO) and omega-3 fatty acids-rich fish oil (O3FO) in the delivery of donepezil hydrochloride microemulsion (DH-ME) to the brain via intranasal route, the present study was conducted. DH:BO and DH:O3FO binary mixtures (9:1 to 1:9) were prepared by simple physical mixing and subjected to in vitro diffusion study. Ratios of DH:BO and DH:O3FO, which showed the highest diffusion, were selected for further development of microemulsion (ME).

Exploring the potential of minoxidil tretinoin liposomal based hydrogel for topical delivery in the treatment of androgenic alopecia.

: Androgenic alopecia (AGA) is a condition of progressive hair loss and involves follicular miniaturization triggered mainly due to varying levels of androgen besides environmental and genetic factors, which may also play some role. Minoxidil (MXD) has been considered as most effective therapeutic moiety to treat this disorder. Another drug Tretinoin (TRET) is known for its comedolytic activity and is reported to enhance percutaneous absorption of MXD.

Fast dissolving electrospun polymeric films of anti-diabetic drug repaglinide: formulation and evaluation.

Repaglinide is a well-known FDA approved drug from category of meglitinide; used for the treatment of diabetes. However, its use is limited because of its poor water solubility which leads to erratic drug absorption. Present work focuses on formulation and evaluation of polyvinyl alcohol (PVA)-polyvinyl pyrrolidone (PVP) nanofibers to counter this problem of poor water solubility.

Cow ghee fortified ocular topical microemulsion; , , and evaluation.

Utility of cow ghee (CG) as permeation enhancer in development of topical ocular microemulsion (ME) for delivery of fluocinolone acetonide (FA) to posterior eye. For ME preparation, oil, surfactant and cosurfactant were screened based on solubility of FA. Pseudoternary phase diagrams were constructed to determine their ratios.

Fatty acids as essential adjuvants to treat various ailments and their role in drug delivery: A review.

Since the discovery of fatty acids, a niche has been carved for their vital role as adjuvants in drug delivery and as treatment for various diseases. The literature has repeatedly described the essential role of various fatty acids in treating a wide range of diseases and disorders, from central nervous system diseases to wound healing. The use of fatty acids has expanded to many horizons and in recent decades they have gained importance as drug delivery adjuvants in addition to their auxiliary benefits in treating various diseases.

A review on recent drug delivery systems for posterior segment of eye.

Eye is the unique sense organ with complex and sophisticated anatomy and physiology. Being most instrumental for vision, it is secured by varied protective barriers; ranging from static (membranous) to dynamic (vascular) barrier. Although these barriers are very efficient to protect eye from exogenous substances and external stress, it is caught by various irreversible vision impairing ailments like cataract, conjunctivitis, glaucoma, uveitis, diabetic retinopathy (DR), diabetic macular edema (DME), age related macular degeneration (AMD), cytomegalovirus (CMV) retinitis, retinitis pigmentosa (RP), retinal vein occlusion (RVO), endophthalmitis affecting both anterior and posterior segment of eye.

Parenteral nanosuspensions: a brief review from solubility enhancement to more novel and specific applications.

Advancements in techniques of lead molecule selection have resulted in the failure of around 70% of new chemical entities (NCEs). Some of these molecules are getting rejected at final developmental stage resulting in wastage of money and resources. Unfavourable physicochemical properties affect ADME profile of any efficacious and potent molecule, which may ultimately lead to killing of NCE at final stage.

A bird's eye view of nanoparticles prepared by electrospraying: advancements in drug delivery field.

Recent analysis of the published data reveals the increasing importance of nanotechnology in the field of drug delivery, especially due to easy modulation of drug release and targeting effect. Various conventional methods including nanoprecipitation, spray drying, solvent evaporation, supercritical fluid extraction and ionotropic gelation are well-explored for lab-scale production of nanoparticles and present their own advantages and limitations. Electrospraying a variant of electrospinning is a method based on the processing of polymeric solutions/melt under high electrical voltage to produce particles of desired nature; post optimization of process parameters.

Nanocrystal-based drug delivery system of risperidone: lyophilization and characterization.

Objective: In the present work nanocrystal-based formulation of risperidone (RIS) was proposed to overcome solubility issue of RIS, while lyophilization technique was used effectively, for conversion of RIS nanosuspension to solid state.

Significance: RIS nanosuspension was developed and stabilized with a combination of polycaprolactone and Pluronic F-68 as stabilizers. With focus on critical parameters like nature of cryoprotectants and effect of eutectic temperature on properties of nanosuspension, the suitability of lyophilization technique in improving the physical stability of prepared nanosuspension was also evaluated.

Microemulsion-based delivery of triamcinolone acetonide to posterior segment of eye using chitosan and butter oil as permeation enhancer: an in vitro and in vivo investigation.

The aim of the study was to formulate a microemulsion (ME) using chitosan (CH) and the butter oil (BO) as a permeation enhancer for targeting drug to the posterior segment of the eye, via topical route. Triamcinolone acetonide (TA) was selected as the model drug since it undergoes extensive first-pass metabolism, leading to poor oral bioavailability of 23%. For optimisation of BO concentration, different ratios of TA:BO were prepared by simple physical mixing in the ratio of 1:9 to 9:1 and diffusion study was performed.

Formulation and In-vivo Pharmacokinetic Consideration of Intranasal Microemulsion and Mucoadhesive Microemulsion of Rivastigmine for Brain Targeting.

Purpose: Presence of tight junctions in blood brain barrier (BBB) pose a major hurdle for delivery of drug and severely affects adequate therapeutic concentration to reach the brain. In present work, we have selected Rivastigmine hydrogen tartrate (RHT), a reversible cholinesterase inhibitor, which exhibits extensive first-pass metabolism, resulting in limited absolute bioavailability (36%). RHT shows extremely low aqueous solubility and poor penetration, resulting in inadequate concentration reaching the brain, thus necessitating frequent oral dosing.

Comparative evaluation of electrospraying and lyophilization techniques on solid state properties of Erlotinib nanocrystals: Assessment of In-vitro cytotoxicity.

Introduction: Erlotinib is a well known FDA approved drug from category of tyrosine kinase inhibitors; used for the treatment of lung cancer. However its use is limited because of its poor water solubility.

Objective: The aim of present work was to improve solubility by developing a stable nanocrystal based drug delivery system of ERL with the aid of sodium lauryl sulfate as potential stabilizer and to carry out comparative evaluation of electrospraying and lyophilization as solidification techniques on its solid state properties.

Electrospun polymeric nanofibers: New horizons in drug delivery.

Nanofibers obtained using electrospinning technique are being used since ages especially in fields of textile industry, sensors, filters, protective clothing and tissue engineering. Their use as drug delivery system is an emerging platform in the field of pharmaceuticals and now-a-days formulation scientists are paying great attention to the technology due to several advantages prime being easy modulation of drug release profile depending upon the properties of polymer/polymeric blends/other materials used. Although there are several reports citing the use of antibiotics-loaded nanofibers as wound dressing materials and as antimicrobial therapy in periodontics; still there is a good scope of expanding the horizon for its application in newer ailments.

Nanocrystal Based Drug Delivery System: Conventional and Current Scenario.

Background: Most of the chemical substances which emerge out as potential drug candidates (Active Pharmaceutical Ingredients) are either weak acids or weak bases. The poor aqueous solubility of these drug substances is a common concern. Several R&D centers are focused on developing suitable, economic, simpler and more feasible solubility enhancement techniques for increasing the solubility and thereby bioavailability of such drug substances.

Non-invasive intranasal delivery of quetiapine fumarate loaded microemulsion for brain targeting: Formulation, physicochemical and pharmacokinetic consideration.

Systemic drug delivery in schizophrenia is a major challenge due to presence of obstacles like, blood-brain barrier and P-glycoprotein, which prohibit entry of drugs into the brain. Quetiapine fumarate (QF), a substrate to P-glycoprotein under goes extensive first pass metabolism leading to limited absorption thus necessitating frequent oral administration. The aim of this study was to develop QF based microemulsion (ME) with and without chitosan (CH) to investigate its potential use in improving the bioavailability and brain targeting efficiency following non-invasive intranasal administration.

"Application of Box-Behnken design for optimization and development of quetiapine fumarate loaded chitosan nanoparticles for brain delivery via intranasal route* ".

The objective of the present investigation was to optimize and develop quetiapine fumarate (QF) loaded chitosan nanoparticles (QF-NP) by ionic gelation method using Box-Behnken design. Three independent variables viz., X1-Concentration of chitosan, X2-Concentration of sodium tripolyphosphate and X3-Volume of sodium tripolyphosphate were taken to investigate their effect on dependent variables (Y1-Size, Y2-PDI and Y3-%EE).