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Modern science has been transformed by open access (OA) publishing levied a significant economic burden on the authors. This article analyzes the discrepancies among OA publication fees in pharmacology, toxicology, and pharmaceutics. The observations comprise 160 OA journals and their corresponding Q ranking, SJR, H index, impact factor, country, and cost of publication. The OA fees were found to depend on the quality matrices, which was unexpected. Differences in OA fees raise ethical questions as OA fees are meant to cover the publication charges by the publishers or generate more revenues by taking advantage of the authors’ temptation to publish in high-impact journals. Despite our findings being based on limited sample size and belonging to a particular field (pharmacy), it will shed considerable light on the issue of discrepancies among APCs charged by OA journals.

Introduction: Indigenous plants have historically been crucial in treating human diseases across various cultures worldwide. Research continues to uncover new therapeutic uses for indigenous plants, from treating infectious diseases to managing chronic conditions such as diabetes and wound care. This study aimed to examine the effect of palm tree leaves "Phoenix dactylifera L" extract and its topical film formulation on wound healing and blood glucose levels. Methods: Palm leaves were collected, authenticated, powdered, and extracted with ethanol by cold maceration. Saponins were isolated. The dried extract was analyzed using reverse-phase high-pressure liquid chromatography to identify the phytochemicals present. Diabetes mellitus was induced by a single intraperitoneal injection of Streptozotocin (40mg/kg). Rats with blood glucose levels ≥ 200 mg/dl were used to determine the reduction in blood glucose with or without the oral extract. Incision and excision wounds were induced in both diabetic and normal rats. Topical films containing extract or saponin and inert films were applied to the wounds every other day, and wound sizes were recorded until the wound was completely healed. Results: The presence of six flavonoids, Naringin, Rutin, Quercetin, Kaempferol, Apigenin, and Catechin, and five phenolic acids, Syringic acid, p Coumaric acid, Caffeic acid, Ferulic acid, Ellagic acid were detected in the dried extract. A significant reduction in blood sugar in diabetic rats and wound diameter in the treated group compared to the control group in both diabetic and normal rats was observed, confirming the promising role of palm leaf extract on diabetes and wound care. Macroscopic, morphometric, and histological data suggested that the cutaneous wound healing in rats treated with the leaf extract was better and faster than the control or inert groups. Conclusions: Our research findings highlight the marked effect of Phoenix dactylifera extract as a supportive or alternative treatment for both hyperglycemia and incision or excision wounds. Further research and clinical trials are warranted to validate these findings and explore the underlying mechanisms of action. [ABSTRACT FROM AUTHOR]

Modern science has been transformed by open access (OA) publishing levied a significant economic burden on the authors. This article analyzes the discrepancies among OA publication fees in pharmacology, toxicology, and pharmaceutics. The observations comprise 160 OA journals and their corresponding Q ranking, SJR, H index, impact factor, country, and cost of publication. The OA fees were found to depend on the quality matrices, which was unexpected. Differences in OA fees raise ethical questions as OA fees are meant to cover the publication charges by the publishers or generate more revenues by taking advantage of the authors' temptation to publish in high-impact journals. Despite our findings being based on limited sample size and belonging to a particular field (pharmacy), it will shed considerable light on the issue of discrepancies among APCs charged by OA journals. [ABSTRACT FROM AUTHOR]

Despite the promising features and aggressive research, the success of nanoparticles in clinical trials is minimal. This manuscript discusses the complex biological barriers that impede the journey of nanoparticles to the target site and the approaches used to overcome them. The '6R' framework (right route, right target, right design, right patient, right combination and right technology) is proposed to improve the clinical translation of nanomedicines. Disease-driven approach contrary to the traditional formulation-driven approach is suggested. Data-driven methods can analyze the relationships between various diseases, patient pathophysiology and the physicochemical properties of different nanomedicines, aiding in the precise selection of the most appropriate treatment options. Further research is needed to evaluate and refine these approaches to develop nanomedicines for clinical success. Plenty of work is happening in the field of nanomedicine, but only a few nanomedicines have hit the market. This could be due to many reasons. One of the major reasons is their complex biology. It is imperative to understand how the body reacts to nanomedicines. Obstacles imposed by the body and ways to overcome them are highlighted in this work. The principles of successful nanomedicine design are discussed. This includes proper selection of route, target, design, patient, combination and technology. A framework for evaluating the success of nanomedicine is also proposed. Nanomedicines should be designed using a disease-driven approach. This will help make nanomedicine more viable. Further research is required to test the validity of the proposed model. [ABSTRACT FROM AUTHOR]

In the contemporary medical model world, the proniosomal system has been serving as a new drug delivery system that is considered to significantly enhance the bioavailability of drugs with low water solubility. The application of this system can improve the bioavailability of aceclofenac that is used for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. The present study is intended to develop an optimized proniosomal aceclofenac formula by the use of different carriers. Aceclofenac proniosomes have been prepared by slurry method, and different carriers such as maltodextrin, mannitol, and glucose were tried. Prepared proniosomes characterized by differential scanning calorimetry (DSC) analysis and Fourier transform infrared (FTIR) analysis revealed the compatibility of the drug chosen with the ingredient added, powder X-ray diffractometry (XRD) confirmed the amorphous phase of the prepared proniosomes, and finally, the surfactant layer was observed by scanning electron microscopy (SEM). Aceclofenac physical state transformations were confirmed with all formulas but maltodextrin proniosomes exhibited solubility more than other formulations. HPLC method has been used to analyze the niosomes derived from proniosomes in terms of their entrapment capability and drug content. The obtained results revealed that aceclofenac proniosomes can be successfully prepared by using different carriers.

Objective: Designing a region's need-based programs can be an exceptional complement boosting the knowledge economy of the country. United Arab Emirates (UAE) is increasingly focusing on the pharma and biotech sectors. As a result, there have been increasing demands for qualifications in pharmacy education to fit into higher roles in pharmaceutical industries and multinational companies (MNCs) in the region. Method: This study is a case demonstration that details the design processes authors used for the graduate program 'Pharmaceutical Product Development'. Results: The three stages in program positioning; identifying the need for the new program, program design, and development, and program effectiveness are illustrated in this manuscript. Conclusion: The authors believe that this manuscript serves as a valuable resource for novice curriculum developers in the development of new educational programs. [ABSTRACT FROM AUTHOR]

This study aimed to evaluate and compare the antihepatotoxicity effect of Fagonia indica extract and its solid dispersion formulation (SD) against paracetamol-induced hepatotoxicity in rats. Dried Ethanolic plant extract was prepared by cold maceration in ethanol followed by solvent evaporation under reduced pressure. Quality control of crude extract was performed and the total phenolic and flavonoid contents were determined. Solid dispersion (SD) formulations were prepared by solvent evaporation technique and optimized with respect to drug solubility. Antihepatotoxicity activities of Fagonia indica extract and optimized solid dispersion were performed against paracetamol-induced hepatotoxicity in rats. Quality control parameters like total ash, acid insoluble ash, water soluble ash, crude fiber content and moisture content were within the acceptable limits. Total flavonoid and phenolic contents were found to be 31.289mg quercetin equivalents/g and 40.28mg gallic acid equivalent/g respectively. TLC Investigation of the plant extract revealed the presence of gallic acid, kaempferol and quarcetin. Optimized SD formulation with 200 mg of the dried extract, 350mg of PEG 4000 and 50mg of Tween 20 showed almost four-fold increasing in the solubility of the extract in water. The average hydrodynamic diameter of extract particles was reduced from 1972 nm to 437.6nm when prepared as SD. SD formulation showed highest antihepatotoxicity activity compared with plain plant extract at the same concentration. Optimized SD formulation at 500mg dose showed complete recovery from hepatotoxicity induced by paracetamol in rats. Therefore, SD is found to be one of the promising strategy to enhance the antihepatoxicity activity of Fagonia indica plant. [ABSTRACT FROM AUTHOR]

Colorectal cancer (CRC) is the third most common malignancy among both the genders globally. Therefore, searching of new therapeutic options is utmost priority. Molecular docking is a widely used tool in drug discovery to identify potential new therapeutic targets. Molecular docking plays a vital role in the visualization of ligand–protein interaction at an atomic level and enhancing our understanding of the ligand behavior thus aiding in the structure-based drug designing. Selected phytochemicals with potential anticancer activities were examined for their binding affinities to the selected VEGFR and EGFR receptors. The receptor protein 3D structures were obtained from Protein Data Bank, and the molecular docking was performed using UCSF Chimera software with its AutoDock Vina tool. Out of 18 compounds screened, Yuanhuanin, Theaflavin, and Genistein have shown highest binding energies. Findings of this study should be further evaluated for their potential use in CRC treatment, management, and prevention. [ABSTRACT FROM AUTHOR]

Introduction: Common cold is the most frequently recurring disease in the world and is a leading cause of doctor visits and missed days from school and work. Cold reliever medicated chewing gum (MCG) will be a definitive patient acceptable solution for this condition. Anti-allergic, cetirizine (CTZ) is a BCS class-I (highly soluble and highly permeable) non-sedating antihistaminic drug and this study was based on the hypothesis that CTZ as a BCS class I drug will be easily released from chewing gum into the salivary fluid within few minutes of chewing and can be easily permeated from oral mucosa by the pressure created by the chewing action and absorbed to a larger extent into the systemic circulation. Therefore, ultimately patients will get quick relief from symptoms of common cold with greater compliance compared to other conventional dosage forms. Materials and Methods: This study mainly focuses on taste masking of CTZ by inclusion complexation method, its formulation development in the MCG form and its quality and performance evaluation with the study of potential factors affecting drug release by 3² full factorial experimental design. A "chew out" study is carried out to assess in vivo drug release from MCG, in which residual amount is extracted from the chewed sample. Results: Formulation ingredients, such as elastomers, softeners, bulking agents, play an important role in the feel of the final product and its consistency; while sweeteners and flavors play a very essential character in its sensory properties. Conclusion: Interindividual variation in chewing frequency and chewing intensity is the main factor which affects release of active ingredient from MCG; while salivary dilution and involuntary swallowing are main reasons for variability in the absorption site, i.e., either from buccal mucosa or from gastrointestinal tract. [ABSTRACT FROM AUTHOR]

The objective of this study was to develop and evaluate squalane oil-containing water-in-oil-in-water (W/O/W) multiple emulsion for mucosal administration of ovalbumin (OVA) as a model candidate vaccine in BALB/c mice. Control and optimized OVA-containing W/O/W emulsion (OVA-Emul) and chitosan-modified W/O/W emulsion (OVA-Emul-Chi) formulations were administered intranasally and orally at an OVA dose of 100 μg. The mucosal and systemic immune responses were evaluated after the first and second immunization. The OVA-Emul formulations resulted in higher immunoglobulin-G (IgG) and immunoglobulin-A (IgA) responses as compared with aqueous solution. In addition, significant IgG and IgA responses were observed after the second immunization dose using the emulsions with both routes of administration. Intranasal vaccination was more effective in generating the systemic OVA-specific IgG response than the mucosal OVA-specific IgA response. Oral immunizations, on the other hand, showed a much higher systemic IgG and mucosal IgA responses as compared with the nasally treated groups. The results of this study show that squalane oil-containing W/O/W multiple emulsion formulations can significantly enhance the local and systemic immune responses, especially after oral administration, and may be adopted as a better alternative in mucosal delivery of prophylactic and therapeutic vaccines. [ABSTRACT FROM AUTHOR]

In the contemporary medical model world, the proniosomal system has been serving as a new drug delivery system that is considered to significantly enhance the bioavailability of drugs with low water solubility. The application of this system can improve the bioavailability of aceclofenac that is used for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. The present study is intended to develop an optimized proniosomal aceclofenac formula by the use of different carriers. Aceclofenac proniosomes have been prepared by slurry method, and different carriers such as maltodextrin, mannitol, and glucose were tried. Prepared proniosomes characterized by differential scanning calorimetry (DSC) analysis and Fourier transform infrared (FTIR) analysis revealed the compatibility of the drug chosen with the ingredient added, powder X-ray diffractometry (XRD) confirmed the amorphous phase of the prepared proniosomes, and finally, the surfactant layer was observed by scanning electron microscopy (SEM). Aceclofenac physical state transformations were confirmed with all formulas but maltodextrin proniosomes exhibited solubility more than other formulations. HPLC method has been used to analyze the niosomes derived from proniosomes in terms of their entrapment capability and drug content. The obtained results revealed that aceclofenac proniosomes can be successfully prepared by using different carriers. [ABSTRACT FROM AUTHOR]

This research work was intended to formulate a novel inhaled product (Budesonide βCD-based NS) for providing the controlled release of Budesonide. [Display omitted] • β-cyclodextrin (βCD), a cyclic oligosaccharide consisting of seven glucose units, was chemically crosslinked with various crosslinking agents such as pyromellitic dianhydride (PMDA), 1, 1′-carbonyldiimidazole (CDI), citric acid (CA), and 1,4-butanediol diglycidyl ether (BDE), and thus βCD-based nanosponges (βCD-NS) were prepared. • Budesonide (BUD) was loaded into five different βCD-NS at four ratios (BUD: NS; 1:1; 1:2; 1:3; 1:4 w:w) using three methods (labelled as methods A, B, and C). CDI-based βCD-NS presented a higher encapsulation efficiency (∼80 %) of BUD at the ratio of BUD: NS 1:3 w:w. • The optimized formulations were successfully characterized by FTIR Spectroscopy analysis, TGA analysis, water absorption capacity (WAC), scanning electron microscopy (SEM), X-ray powder diffraction studies (XRD), and by the measurement of the particle size, zeta potential, encapsulation efficiency, in vitro and in vivo release studies, in vitro/ in vivo correlation and in vitro cytotoxicity on alveolar cells, acute toxicity study, solid-state characterization, and aerosol performance suggesting the potential role of βCD-NS as a pulmonary drug delivery carrier. • In vivo animal studies proposed sustained drug release in the lungs for 12 h which may result in reduced dosing frequency and improved patient convenience and compliance. Budesonide (BUD) is a glucocorticosteroid used to treat chronic obstructive pulmonary disease. Despite this, it is a hydrophobic compound with low bioavailability. To address these hurdles, non-toxic and biocompatible βcyclodextrin-based nanosponges (βCD-NS) were attempted. BUD was loaded on five different βCD-NS at four different ratios. NS with 1,1′-carbonyldiimidazole (CDI) as a crosslinking agent, presented a higher encapsulation efficiency (̴ 80%) of BUD at 1:3 BUD: βCD-NS ratio (BUD-βCD-NS). The optimized formulations were characterized by Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), water absorption capacity (WAC), scanning electron microscopy (SEM), X-ray powder diffraction studies (XRD), particle size, zeta potential, encapsulation efficiency, in vitro and in vivo release studies, acute toxicity study, solid-state characterization, and aerosol performance. In vitro-in vivo correlation and cytotoxicity of the formulations on alveolar cells in vitro were further determined. In vitro and in vivo studies showed almost complete drug release and drug absorption from the lungs in the initial 2 h for pure BUD, which were sustained up to 12 h from BUD loaded into nanosponges (BUD-βCD-NS). Acute toxicity studies and in vitro cytotoxicity studies on alveolar cells proved the safety of BUD-βCD-NS. Several parameters, including particle size, median mass aerodynamic diameter, % fine particle fraction, and % emitted dose, were evaluated for aerosol performance, suggesting the capability of BUD-βCD-NS to formulate as a dry powder inhaler (DPI) with a suitable diluent. To sum up, this research will offer new insights into the future advancement of βCD-NS as drug delivery systems for providing controlled release of therapeutic agents against pulmonary disease. [ABSTRACT FROM AUTHOR]

Introduction: This invention reports the solubilization of Acetaminophen (ACM) within the Povidone (PVP K30) in the solid state for the first time., Methods: First-generation solid dispersions (SDs) were attempted with a different ratio of PVP K:30:ACM. SDs prepared were transparent, suggesting a solid solution (SS) formation, which was a serendipitous discovery. A minimum ratio of 1.25:1 PVP K30: ACM was required to form stable SS, suggesting discontinuous SS. A computational complex prediction tool, fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) confirmed the SS formation., Results: The oral strip formulation was developed from the PVP K30: ACM SS using Polyvinyl alcohol as a film-former found to be optimum concerning physicochemical properties, offering rapid drug dissolution and taste masking., Conclusion: The designed strip is suitable for delivering a child's dose (100-150 mg). However, the developed SS can be formulated as tablets, capsules, or oral dissolving tablets to deliver adult doses with improved therapeutic benefits and patient compliance., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Improved bioavailability of Aceclofenac (ACE) may be achieved through proniosomes, which are considered as one of the most effective drug delivery systems and are expected to represent a valuable approach for the development of better oral dosage form as compared to the existing product. However, the carrier in this system plays a vital role in controlling the drug release and modulating drug dissolution. Accordingly, a comparative study on different carriers can give a clear idea about the selection of carriers to prepare ACE proniosomes., Objective: This study aims to evaluate the role of maltodextrin, glucose, and mannitol as carriers for in vitro and in vivo performance of Aceclofenac (ACE) proniosomes., Methods: Three formulations of proniosomes were prepared by the slurry method using the 100 mg ACE, 500 mg span 60, 250 mg cholesterol with 1300mg of different carriers, i.e., glucose (FN1), maltodextrin (FN2), and mannitol (FN3). In vitro drug release studies were conducted by the USP paddle method, while in vivo studies were performed in albino rats. Pure ACE was used as a reference in all the tests. Lastly, the results were analyzed using the High-Pressure Liquid Chromatography (HPLC) method, and data were evaluated using further kinetic and statistical tools., Results: No significant differences (p > 0.05) in entrapment efficiency (%EE) of FN1, FN2, and FN3 (82 ± 0.5%, 84 ± 0.66%, and 84 ± 0.34% respectively) were observed and formulations were used for further in vitro and in vivo evaluations. During in vitro drug release studies, the dissolved drug was found to be 42% for the pure drug, while 70%, 17%, and 30% for FN1, FN2, and FN3, respectively, at 15 min. After 24 hrs, the pure drug showed a maximum of 50% release while 94%, 80%, and 79% drug release were observed after 24 hr for FN1, FN2, and FN3, respectively. The in vivo study conducted on albino rats showed a higher Cmax and AUC of FN1 and FN2 in comparison with the pure ACE. Moreover, the relative oral bioavailability of proniosomes with maltodextrin and glucose as carriers compared to the pure drug was 183% and 112%, respectively. Mannitol- based formulation exhibited low bioavailability (53.7%) that may be attributed to its osmotic behavior., Conclusion: These findings confirm that a carrier plays a significant role in determining in vitro and in vivo performance of proniosomes and careful selection of carrier is an important aspect of proniosomes optimization., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: In order to prove the validity of a new formulation, a considerable amount of effort is required to study bioequivalence, which not only increases the burden of carrying out a number of bioequivalence studies but also eventually increases the cost of the optimization process., Objective: The aim of the present study was to develop sustained release matrix tablets containing diclofenac sodium using natural polymers and to demonstrate step by step process of product development till the prediction of in vivo marketed product equivalence of the developed product., Method: Different batches of tablets were prepared by direct compression. In vitro drug release studies were performed as per USP. The drug release data were assessed using model-dependent, modelindependent and convolution approaches., Results: Drug release profiles showed that extended release action were in the following order: Gum Tragacanth > Sodium Alginate > Gum Acacia. Amongst the different batches prepared, only F1 and F8 passed the USP criteria of drug release. Developed formulas were found to fit Higuchi kinetics model with Fickian (case I) diffusion-mediated release mechanism. Model- independent kinetics confirmed that total of four batches were passed depending on the similarity factors based on the comparison with the marketed Diclofenac. The results of in vivo predictive convolution model indicated that predicted AUC, Cmax and Tmax values for batch F8 were similar to that of marketed product., Conclusion: This study provides simple yet effective outline of pharmaceutical product development process that will minimize the formulation development trials and maximize the product success in bioequivalence studies., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)

Introduction: Oral-controlled and modified-release drug delivery systems with zero-order sustained-release kinetics have been developed and proven suitable for meeting increasingly sophisticated therapeutic needs. Nevertheless, the impact of basic chronobiology concepts on the practice of medicine is still ongoing and to address chronotherapy needs, various types of pulsatile drug delivery systems have been innovated. The purpose of this review is to highlight these innovations in the field of chronotherapy., Areas Covered: The present review discusses in depth on recent patents and developments related to pulsatile drug delivery systems with eroding, soluble or rupturable barrier coatings, and systems with capsular structures. Besides focusing on all recent innovations, the review addresses the novelty and feasibility of all upcoming technologies being exploited considering pulsatile drug delivery systems., Expert Opinion: There has been a growing interest in pulsatile delivery, which generally refers to the liberation of drugs following a programmable and well-defined lag phase from the time of administration. From 1981 until the present date, patent publications related to pulsatile drug delivery have shown more promising systems with numerous developments in arena of drug delivery. Future development of chronotherapeutic medications requires proper assessment and integration with other emerging disciplines such as hydrogel and transdermal delivery systems. The selection of the appropriate chronopharmaceutical technology should take into considerations with the ease of manufacturing and the cost-effectiveness.

Introduction: Disease management of outdoor patients is mainly affected by patient compliance to the drug therapy, which in turn is governed by patient convenience. Failure to follow through with a treatment decision is one of the biggest causes of unsuccessful medical care. At present, different formulation options are available for various drugs, and hence, the decision is based on the most convenient dosage form for the patient, along with optimum therapeutic benefits., Areas Covered: This paper reviews various available formulation approaches, in the hope of improving patient convenience, compliance and the overall outcome of oral drug therapy., Expert Opinion: While parenterals are valued for their speed and efficiency of delivery, these systems generally score low on patient satisfaction surveys. The oral route is the preferred route for drug delivery, although it renders multiple obstacles to formulate a patient-convenient platform, such as unfavorable taste and swallowing difficulties. Transdermal drug delivery also provides high patient satisfaction, but is effective only for the delivery of smaller, lipophilic molecules. The increasing development of biopharmaceutical therapies renders an increasing number of challenges for formulation scientists to develop a more patient-convenient means of drug delivery.

Over the past several years, immunization and treatment of infectious diseases has undergone a paradigm shift. Stemming from the vaccine research and development, not only a large number of disease-specific vaccines have been developed, but also enormous efforts have been made to improve the effectiveness of vaccines in order to provide optimal immunization. Introduction of nanotechnology and the development of nanocarrier-based vaccines have started to receive a lot of attention in order to provide effective immunization through better targeting and by triggering antibody response at the cellular level. Also, in the past several years, attention is placed on routes of vaccine administration in order to induce both mucosal and systemic immunity against the pathogen. Through judicious selection of the nanocarrier systems and the vaccine antigen, an optimal immunization and protection can be induced. This review article focuses on the patented applications of nanocarrier-based vaccine formulations and delivery. We have examined the United States patent literature to select inventions that specifically address this strategic approach for prevention of infectious diseases.

Many drugs are not being effectively and efficiently delivered using conventional drug delivery approach to brain or central nervous system (CNS) due to its complexity. The brain and the central nervous system both have limited accessibility to blood compartment due to a number of barriers. Many advanced and effective approaches to brain delivery of drugs have emerged in recent years. Intranasal drug delivery is one of the focused delivery options for brain targeting, as the brain and nose compartments are connected to each other via the olfactory route and via peripheral circulation. Realization of nose to brain transport and the therapeutic viability of this route can be traced from the ancient times and has been investigated for rapid and effective transport in the last two decades. Various models have been designed and studied by scientists to establish the qualitative and quantitative transport through nasal mucosa to brain. The development of nasal drug products for brain targeting is still faced with enormous challenges. A better understanding in terms of properties of the drug candidate, nose to brain transport mechanism, and transport to and within the brain is of utmost importance. This review will discuss some pertinent issues to be considered and challenges to brain targeted intranasal drug delivery. A few marketed and investigational drug formulations will also be discussed.

The brain is a delicate organ, and evolution built very efficient ways to protect it. Unfortunately, the same mechanisms that protect it against intrusive chemicals can also frustrate therapeutic interventions. Many existing pharmaceuticals are rendered ineffective in the treatment of cerebral diseases due to our inability to effectively deliver and sustain them within the brain. General methods that can enhance drug delivery to the brain are, therefore, of great interest. Despite aggressive research, patients suffering from fatal and/or debilitating central nervous system (CNS) diseases, such as brain tumors, HIV encephalopathy, epilepsy, cerebrovascular diseases and neurodegenerative disorders, far outnumber those dying of all types of systemic cancer or heart disease. The clinical failure of much potentially effective therapeutics is often not due to a lack of drug potency but rather to shortcomings in the method by which the drug is delivered. Treating CNS diseases is particularly challenging because a variety of formidable obstacles often impede drug delivery to the brain and spinal cord. By localizing drugs at their desired site of action one can reduce toxicity and increase treatment efficiency. In response to the insufficiency in conventional delivery mechanisms, aggressive research efforts have recently focused on the development of new strategies to more effectively deliver drug molecules to the CNS. This review intends to detail the recent advances in the field of brain-targeting, rational drug design approach and drug delivery to CNS. To illustrate the complexity of the problems that have to be overcome for successful brain targeting, a brief intercellular characterization of the blood-brain barrier (BBB) is also included.

Purpose: A niosome based transdermal drug delivery system of Nimesulide (NIM) was developed and extensively characterized and evaluated for in-vitro performance followed by in-vivo evaluation in rats by carrageenan induced rat paw edema method., Method: Niosomes were prepared by lipid film hydration technique using tweens and spans. Preparation of niosomes was optimized for highest percent drug entrapment (PDE). The prepared niosomes were incorporated into 1 percent carbopol gel base and the system was evaluated for drug diffusion across human cadaver skin (HCS) using modified validated diffusion cell. The drug retention studies in niosomes were performed at refrigerated temperature (2 degrees C - 8 degrees C) and at room temperature (25 degrees C+/-2 degrees C) for the period of 2 months. In-vivo performance of plain drug gel, niosomally-entrapped drug in carbopol gel base and marketed formulation were evaluated using acute rat paw edema method., Results: Highest mean percentage edema inhibition (PEI) was observed for niosomal nimesulide gel after 24 hours i.e. 66.68 percent +/- 5.19 percent compared to plain drug gel i.e. 12.57 percent +/- 1.78 percent and marketed NIM formulation i.e. 20.49 percent +/- 0.91 percent., Conclusion: Findings of this investigation conclusively demonstrate prolongation of drug release and increase in amount of drug retention into the skin and permeation across the skin after niosomal encapsulation of NIM. Developed nimesulide niosomal gel formulation has also demonstrated enhanced anti-inflammatory activity compared to plain drug gel and marketed formulation.