Saffron (Crocus sativus L.) extract attenuates chronic scopolamine-induced cognitive impairment, amyloid beta, and neurofibrillary tangles accumulation in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Crocus sativus L. known as saffron, is a popular food condiment with a high aroma, deep colour, and long and thick threads (stigmas) cultivated in Iran, Morocco, Spain, Italy, China, Japan, France, Turkey, and India. In 'Ayurveda', saffron is acknowledged for its immunostimulant, aphrodisiac, cardiotonic, liver tonic, nervine tonic, carminative, diaphoretic, diuretic, emmenagogue, galactagogue, febrifuge, sedative, relaxant, and anxiolytic activities. The renowned Persian physician and philosopher, Avicenna, delineated saffron as an antidepressant, hypnotic, anti-inflammatory, hepatoprotective, bronchodilator, and aphrodisiac in his book, the Canon of Medicine. Within traditional Iranian Medicine (TIM), saffron is characterized as a mood elevator and a rejuvenator for the body and senses. Further, the ethnopharmacological evidence indicates that saffron has shown an effect against neurodegenerative disorders namely, dementia, Alzheimer's, and Parkinson's with its bioactive constituents i.e., carotenoids and apocarotenoids. AIM: The present study aimed to investigate the potential of standardized (Kashmir Saffron, India) Crocus sativus extract (CSE) in chronic scopolamine-induced cognitive impairment, amyloid beta (Aß) plaque, and neurofibrillary tangles (NFT) accumulation in rat brains by targeting AChE inhibition and scopolamine mechanistic effect. METHODS: The experimental animals were divided into six groups: group 1: normal control, group 2: scopolamine, group 3,4 and 5 rivastigmine tartrate, CSE (p.o. 10 mg/kg, 15 mg/kg, and 20 mg/kg) respectively. Each treatment group received scopolamine after 20 min of dosing, till 4 weeks. The effects of different treatments on learning, acquisition, and reversal memory were performed using a Morris water maze test. In addition to behavioral assessments, biochemical parameters such as AChE, IL-6, and antioxidants were measured in isolated brains. Histological observations were also conducted to assess the presence of Aß plaques and NFT. Furthermore, molecular docking was performed to explore the potential AChE inhibitory activity of the bioactive constituents of standardized CSE. RESULTS: Scopolamine produces memory impairment, and its chronic administration forms Aß plaque and NFT in rat brains. Supplementation with CSE in presence of scopolamine has shown remarkable effects on behavioural activity, special acquisition, and reversal memory. The CSE has also shown promising effects on AChE inhibition and antioxidant activity. The results of the docking study also indicate that trans-crocetin, i.e., a biologically active metabolite of Crocins, has strong AChE inhibitory activity, supported by an in vivo animal experiment. CONCLUSION: Supplementation with CSE significantly attenuates the formation of Aß plaque and NFT in the hippocampus at a dose of 20 mg/kg per day. In addition, CSE also counters scopolamine-induced neuroinflammation.

Quantum Dot-based Bio-conjugates as an Emerging Bioimaging Tool for Cancer Theranostic- A Review.

Cancer is the most widely studied disorder in humans, but proper treatment has not yet been developed for it. Conventional therapies, like chemotherapy, radiation therapy, and surgery, have been employed. Such therapies target not only cancerous cells but also harm normal cells. Conventional therapy does not result in specific targeting and hence leads to severe side effects. The main objective of this study is to explore the QDs. QDs are used as nanocarriers for diagnosis and treatment at the same time. They are based on the principle of theranostic approach. QDs can be conjugated with antibodies via various methods that result in targeted therapy. This results in their dual function as a diagnostic and therapeutic tool. Nanotechnology involving such nanocarriers can increase the specificity and reduce the side effects, leaving the normal cells unaffected. This review pays attention to different methods for synthesising QDs. QDs can be obtained using either organic method and synthetic methods. It was found that QDs synthesised naturally are more feasible than the synthetic process. Top or bottom-up approaches have also emerged for the synthesis of QDs. QDs can be conjugated with an antibody via non-covalent and covalent binding. Covalent binding is much more feasible than any other method. Zero-length coupling plays an important role as EDC (1-Ethyl-3-Ethyl dimethylaminopropyl)carbodiimide is a strong crosslinker and is widely used for conjugating molecules. Antibodies work as surface ligands that lead to antigen- antibody interaction, resulting in site-specific targeting and leaving behind the normal cells unaffected. Cellular uptake of the molecule is done by either passive targeting or active targeting. QDs are tiny nanocrystals that are inorganic in nature and vary in size and range. Based on different sizes, they emit light of specific wavelengths. They have their own luminescent and optical properties that lead to the monitoring, imaging, and transport of the therapeutic moiety to a variety of targets in the body. The surface of the QDs is modified to boost their functioning. They act as a tool for diagnosis, imaging, and delivery of therapeutic moieties. For improved therapeutic effects, nanotechnology leads the cellular uptake of nanoparticles via passive targeting or active targeting. It is a crucial platform that not only leads to imaging and diagnosis but also helps to deliver therapeutic moieties to specific sites. Therefore, this review concludes that there are numerous drawbacks to the current cancer treatment options, which ultimately result in treatment failure. Therefore, nanotechnology that involves such a nanocarrier will serve as a tool for overcoming all limitations of the traditional therapeutic approach. This approach helps in reducing the dose of anticancer agents for effective treatment and hence improving the therapeutic index. QDs can not only diagnose a disease but also deliver drugs to the cancerous site.

Bio-Functional Mesoporous Silica Nanoparticles as Nano-Structured Carriers in Cancer Theranostic Review on Recent Advancements.

BACKGROUND: Cancer is a life-threatening disease worldwide, but proper treatment has not yet been developed. Many therapies are available to treat cancer disorders, like chemotherapy, surgery, hormone therapy, and immunotherapy. Chemotherapy often relies on a combination of harmful, highly toxic platinum-based compounds. Also, there are chances of poor distribution of chemotherapeutic agents and cytotoxic to most cells which leads to damage to other healthy cells, also, there are chances of resistance. OBJECTIVE: The main objective of this study is the development of mesoporous silica nanoparticles. Mesoporous silica nanoparticles are recognized as carriers with high drug loading capacity and significant functionalized surface area for targeted drug delivery. Mesoporous silica nanoparticles have shape, particle size, pore volume, higher surface area, and the possibility of surface modification. Hence results in thermally and chemically stable nanomaterials. For targeted drug delivery, MSN is conjugated with a variety of ligands, including monoclonal antibodies, hyaluronic acid, transferrin, folic acid, etc., that have a particular affinity for the receptors that are overexpressed on the surface of malignant cells, so using this nanocarrier reducing the dose related toxicity of normal cell. METHODS: This review focuses on different methods for synthesizing mesoporous silica nanoparticles. Sol-gel method and modified stobber method were used for the synthesis of this nanoparticle. RESULTS: Successfully synthesized mesoporous silica nanoparticle with particle size around 50-200 nm and drug loading efficiency was found to be around 71%. CONCLUSION: Mesoporous silica nanoparticles are great carriers for intracellular and targeted drug delivery systems.

Development and Validation of SI/RS-UHPLC-PDA Method for Olmesartan Medoxomil and Metoprolol Succinate-Related Substance.

Objectives: Olmesartan medoxomil (OLM) and metoprolol succinate (MPS) in fixed-dose combination (FDC) tablet formulation prescribed extensively. Stability indicating (SI) method for impurities and related substance (RS) test quantitates the amount of these analytes in formulation; the manuscript presents SI/RS-ultra-high performance liquid chromatography-photodiode array (UHPLC-PDA) method for OLM and MPS and their impurities. Materials and Methods: Well-resolved separation of all analytes was achieved with gradient elution on a Shimadzu on Shimpack GIST-C18 (100 mm x 2.1 mm, 2 µm) column maintained at 25°C. Mobile phase-A consist of 0.1% orthophosphoric acid in water and mobile phase-B was acetonitrile at a flow rate of 0.4 mL/min, data integrated at 225 nm and 16 min of short runtime for satisfactory elution of all peaks. Results: The proposed SI/RS-UHPLC-PDA method was developed and validated as per International Conference on Harmonisation (ICH) of Technical Requirements guidelines. The system suitability test complied by all eluted peaks of the interest with acceptable linearity, recovery, and precision. Specificity, robustness, and method sensitivity parameters were determined; all the parameters were found to be within the limits. All the impurities and stress-degraded peaks were well resolved. Conclusion: The proposed method was found to be simple, fast, linear, and accurate. Further, the method is precise, robust, and specific; suitable for routine IPQC during active pharmaceutical ingredient manufacturing, stability and impurity profiling studies of the titled bulk analytes. Furthermore, the method can be extended to assess the levels of impurities formed during life cycle of new FDCs of titled analytes.

Detailed Review on Gestational Diabetes Mellitus with Emphasis on Pathophysiology, Epidemiology, Related Risk Factors, and its Subsequent Conversion to Type 2 Diabetes Mellitus.

Any degree of glucose intolerance during the pregnancy of a women is termed as Gestational Diabetes Mellitus (GDM). It may further develop into Type 2 Diabetes Mellitus (T2DM) later in life. GDM affects both mother and infant in multiple ways and there are various factors that predispose the development of GDM.The primary objective of this review is to describe the various aspects related to GDM and the subsequent risk of developing T2DM later in life.We reviewed freely accessible, full-text articles, available in PubMed, Google Scholar, and MEDLINE in the English language, till August 2022 pertaining to GDM.The pathophysiology of underlying glucose intolerance has been discussed, including the various factors like ß-Cell dysfunction, chronic insulin resistance, adiponectin, insulin resistance. GDM affects pregnancies world-wide, but it is higher in the South-east Asia, northern America and Caribbean, south and central America regions. Along with ethnicity, various modifiable and non-modifiable risk factors also play a major role in development of disease. Although no standard diagnostic criteria is accepted world-wide for screening of GDM, but the one-step and two-step approach has made quite a difference. The risk of developing T2DM after GDM is well documented, and it increases with age. GDM leads to an onset of diabetes in the family at a young age, it leads to poor consequences on the health of both the mother and infant. Standard diagnostic criteria, proper education and counselling of the mother is required to tackle the condition.

Beneficial effect of polyherbal formulation in letrozole induced Polycystic ovarian syndrome (PCOS).

Aim of the study: PCOS is an endocrine condition that results in enlarged ovaries with tiny cysts on the margins. The present study aims to investigate the beneficial effect of polyherbal formulation in Letrozole induced PCOS in female Albino Wistar rats. Materials and methods: Acute toxicity study of the polyherbal formulation by administering a single dose (2000 mg/kg) was done in female Albino Wistar rats (20 weeks, 250 g) following OECD guideline 423. For PCOS induced study female Albino Wistar rats were divided into six groups (6 animals/group). Group I (control) was given 0.5% carboxymethylcellulose (CMC) suspension daily as vehicle control. Letrozole (1 mg/kg) was orally administered for 21 days in Group II to VI for induction of PCOS. After induction of PCOS, animals were treated with standard drug (Group III- Clomiphene citrate- 1 mg/kg) and polyherbal tablets (Group IV - 500 mg/kg, Group V- 750 mg/kg, and Group VI - 1000 mg/kg) up to 50 days. Vaginal smears were taken daily to check the estrous cycle. Body weight was measured weekly. Blood samples were withdrawn on 0,21 and 50 days for the determination of fasting blood glucose, lipid profile, LH, FSH, and hormonal levels. Results: Administration of letrozole caused the abnormality in serum sex hormone profile, lipid profile, glucose, and the estrous cycle. The treatment with polyherbal formulation significantly decreased (P < 0.0001) the level of testosterone and improved estradiol and progesterone levels (P < 0.0001). There was a decrease in elevated glucose levels from 71.51 ± 0.15 mg/dl in disease induced group to 57.33 ± 1.90 mg/dl in treatment groups. The triglycerides level was normalized to 33.41 ± 1.81 mg/dl and HDL level was increased to 40.63 ± 1.35 mg/dl in treatment groups. The polyherbal formulation by exerting its beneficial effect also caused the disappearance of the cysts in the ovaries. Conclusion: The polyherbal formulation was found to be effective in PCOS. The effect may be attributed to the individual herbs reported having a significant effect on the pathophysiology of letrozole induced PCOS.

A Perspective on EGFR and Proteasome-based Targeted Therapy for Cancer.

BACKGROUND: Cancer is known to be the most leading cause of death worldwide. It is understood that the sources causing cancer mainly include the activity of endogenous oncogenes, nonviral compounds and the fundamental portion of these oncogenes; the tyrosine kinase activity and proteasome activity are the main biomarkers responsible for cell proliferation. These biomarkers can be used as main targets and are believed to be the 'prime switches' for the signal communication activity to regulate cell death and cell cycle. Thus, signal transduction inhibitors (ligandreceptor tyrosine kinase inhibitors) and proteasome inhibitors can be used as a therapeutic modality to block the action of signaling between the cells as well as protein breakdown in order to induce cell apoptosis. AIMS: This article highlights the key points and provides an overview of the recent patents on EGFR and proteosome-based inhibitors having therapeutic efficacy. This review focuses on the patents related to therapeutic agents, their preparation process and the final outcome. OBJECTIVE: The main objective of this study is to facilitate the advancement and current perspectives in the treatment of cancer. CONCLUSION: There are numerous strategies discussed in these patents to improve the pharmacokinetics and pharmacodynamics of EGFR and proteasome inhibitors. Further, the resistance to targeted therapy after long-term treatment can be overcome by using various excipients that can be used as a strategy to carry the drug. However, there is a need and scope for improving targeted therapeutics for cancer treatment with better fundamentals and characteristics. The widespread research on cancer therapy can create the path for future advancements in therapy with more prominent outcomes.

Preparation and Optimization of Leuprolide Acetate Nanoparticles Using Response Surface Methodology: In Vitro and Ex Vivo Evaluation.

This study aims to develop optimized leuprolide acetate (LA) nanoparticles (NPs) for intranasal delivery in the treatment of Alzheimer's disease. Box-Behnken Design was used to optimize LA polylactide-co-glycolic acid (PLGA) NPs. The independent variables chosen were PLGA concentration, surfactant concentration, and the ratio of water to oil phase, whereas the dependent variables were particle size and % entrapment efficiency. The optimized NPs were evaluated by in vitro drug release study, ex vivo diffusion study, histopathology study, hemolytic stability study, and stability in simulated nasal fluid (SNF). The optimized NPs had particle size of 182.6 ± 1.5 nm, polydispersity index (0.3), % entrapment efficiency (77.3 ± 0.6), and zeta potential (-5.6 mv ±0.2). The in vitro drug release indicated 96% of pure drug release in 6 h, whereas only 66.35% of the drug was released from the optimized formulation at 48 h. The ex vivo diffusion study indicated an apparent permeability coefficient of 5.0 + 0.3 × 104 for drug-containing NPs, which was higher than for plain drug solution (2.0 + 0.2 × 104). Sheep nasal toxicity and hemolytic study proved the safety of formulation. The optimized NPs were found to be stable in SNF. Thus, nanoparticulate formulation of LA was optimized by quality by design approach.

Development of Bromfenac Sodium Loaded Pluronic Nanomicelles: Characterization and Corneal Permeation Study.

BACKGROUND: The Cataract is the leading cause of visual impairment and preventable blindness worldwide. Cataract removal surgery involves various post-operative complications like pain and inflammation. OBJECTIVES: The objective of this study is to screen the polymer concentration as well as optimize the formulation components to develop the pluronic micelles with nanosized characterization and for enhanced corneal permeation study. METHODOLOGY: For optimization, Central Composite design was employed to study the effect of independent variables, concentration of Pluronic F 127 (X1) and the concentration of Hyaluronic acid (X2) on chosen responses (Y 1 ) Micelle size, (Y 2 ) Entrapment Efficiency, (Y 3 ) Viscosity. The lyophilised powder was used for physical characterisation. RESULTS: The formulation containing 5%w/v Pluronic F127 and 0.2%w/v Hyaluronic acid was the optimised composition with micelle size and zeta potential 38.74±4.12nm and -17.6±0.1 mV respectively. In-vitro drug release was found to be 91.72±1.2 percentage in 8 hours. Surface morphology revealed micelles were spherical in shape. Ocular irritancy study showed that formulation was safe and non-irritant. In vitro corneal permeation studies through excised rabbit cornea indicated 1.5 fold increase in ocular availability without corneal damage compared to an aqueous suspension containing the same amount of drug in nanomicelles. CONCLUSION: In a nutshell, Pluronic Nanomicelles would be a platform for the delivery of Bromfenac Sodium.

Pemetrexed - First-Line Therapy for Non-Squamous Non-Small Cell Lung Cancer: A Review of Patent Literature.

BACKGROUND: Pemetrexed is a folate analogue metabolic inhibitor for mammalian cells. Pemetrexed is toxic to several cancer cells by interfering with their new biosynthesis of nucleotides, thus causing cell apoptosis. Presently, Pemetrexed is given to patients with Non-Small Cell Lung Cancer (NSCLC). OBJECTIVE: This review focuses on the recent patents of Pemetrexed. This assessment includes patents grouped in segments like crystalline form patent, composition related patents, product patents, as well as a method of treatment. The aim of this review is to simplify inventors with existing patents in a single place. METHODS: Data were searched from several available databases, including paid databases which include Orbit® and SciFinder®. Free databases include Worldwide Espacenet® (EPO), Patentscope® (WIPO), InPASS (Indian patent database) and Google Patents. RESULTS: Some new polymorph and composition-related inventions of Pemetrexed have been recently patented as its orange-book listed patents will soon expire in May 2022. Further, because of the problem of oxidation through the development and continuing storage of Pemetrexed composition, several excipients are experimented with within these patents to stabilize the same. Nevertheless, there is a need for further development of an improved composition of Pemetrexed with improved characteristics. CONCLUSION: Wide research has been conducted on different processes for preparing Pemetrexed and formulation thereof. Such type of active research may clear the track for the generic companies in the United States, producing the formulation at low prices and providing universal health care at economical prices.

Bortezomib - First Therapeutic Proteasome Inhibitor for Cancer Therapy: A Review of Patent Literature.

BACKGROUND: Bortezomib is a reversible inhibitor of proteasome proteins in mammalian cells. Bortezomib is proven to be cytotoxic to a number of tumor cells by disrupting their normal homeostatic mechanism and thereby, causing cell death. Currently, Bortezomib is prescribed for patients with multiple myeloma and mantle cell lymphoma. OBJECTIVE: This assessment highlights the overview of the recent patents of Bortezomib. This review includes patents grouped in sections like product patents, process patent, composition related patents as well as the treatment methodology. The objective of this article is to facilitate researchers with all existing patents at a single place. METHODS: Data were searched from various online databases. In which, paid databases include SciFinder® and Orbit®. Free databases include Patentscope® (WIPO), Worldwide Espacenet® (EPO), Google Patents and InPASS (Indian patent database). RESULTS: Several new processes and composition related patents of Bortezomib have been recently patented as its orange-book listed patents are going to soon expire during July 2022. Further, due to the problem of oxidation during development and long-term storage of Bortezomib formulation, a number of excipients are tried in these patents to stabilize the same. However, there is still a need for further development of an improved formulation of Bortezomib with better characteristics. CONCLUSION: Extensive research has been carried out on various processes for preparing Bortezomib and the composition thereof. This type of dynamic research will clear the path for many generic players in the United States, which lead to the reduction of the price of the composition and thereby enhancing global health care at cheaper prices.

Application of Failure Mode Effect Analysis in Wurster-Based Pelletization Technology: a Technical Note.

The deployment of oral multi-unit pellet formulation has gained significant attention in recent years conferring to numerous applications, especially in achieving modified release and acid resistance property. The fluidized bed coating, specifically Wurster technique is commercially utilized for pellet manufacturing, which is a complex process involving too many variables. Risk assessment tools can be employed to determine the critical variables affecting the pre-defined quality profile and screen out important parameters out of literally hundreds of variables to develop a robust product. The present review aims to describe possibly all the variables involved in Wurster coating process and application of FMEA in pellet manufacturing. A brief case study regarding applicability of FMEA to study the effects of critical factors is outlined. Risk assessment tools assist to reduce number of trials to manageable levels with aid of prior art, literature, and preliminary trials to develop an optimized product.

Solubility Enhancement of Budesonide and Statistical Optimization of Coating Variables for Targeted Drug Delivery.

The purpose of the research was to present Budesonide (BUD) as a novel formulation showing improved aqueous solubility, which may decrease variability in C max⁡ and T max⁡ found in inflammatory bowel disease (IBD) patients, and drug targeting to colon. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The SD was used to prepare tablet equivalent to 9 mg of BUD. The tablet was coated with enteric polymers Eudragit S100 and Eudragit L100 to target colon. The ratio of polymers and percentage coating was optimized using statistical design. Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release. Dissolution at different pH showed that drug release in colon could be modified by optimizing the ratio of polymers and percentage coating. The dissolution data showed that the percentage coating and ratio of polymers are very important to get lag time and optimum formulation. The optimized batch from statistical design was kept under accelerated condition for three months. After accelerated stability study, there was no significant change in the drug release.

Preparation and evaluation of agglomerated crystals by crystallo-co-agglomeration: an integrated approach of principal component analysis and Box-Behnken experimental design.

Poor mechanical properties of crystalline drug particles require wet granulation technique for tablet production which is uneconomical, laborious, and tedious. The present investigation was aimed to improve flow and mechanical properties of racecadotril (RCD), a poorly water soluble antidiarrheal agent, by a crystallo-co-agglomeration (CCA) technique. The influence of various excipients and processing conditions on formation of directly compressible agglomerates of RCD was evaluated. Principal component analysis and Box-Behnken experimental design was implemented to optimize the agglomerates with good micromeritics and mechanical properties. The overall yield of the process was 88-98% with size of agglomerates between 351 and 1214 µm. Further, higher rotational speed reduced the size of agglomerates and disturbed sphericity. The optimized batch of agglomerates exhibited excellent flowability and crushing strength. The optimized batch of RCD agglomerates was characterized by fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry and gas chromatography which illustrated absence of drug-excipient interaction with minimal entrapment of residual solvent. Hence, it may be concluded that both excipients and processing conditions played a vital role to prepare spherical crystal agglomerates of RCD by CCA and it can be adopted as an excellent alternative to wet granulation.

Influence of excipients and processing conditions on the development of agglomerates of racecadotril by crystallo-co-agglomeration.

PURPOSE: The purpose of the present investigation was to improve the flow and mechanical properties of racecadotril by a crystallo-co-agglomeration (CCA) technique. Direct tableting is a requirement of pharmaceutical industries. Poor mechanical properties of crystalline drug particles require wet granulation which is uneconomical, laborious, and tedious. MATERIALS AND METHODS: The objective of this work was to study the influence of various polymers/excipients and processing conditions on the formation of directly compressible agglomerates of the water-insoluble drug, racecadotril, an antidiarrheal agent. The agglomerates of racecadotril were prepared using dichloromethane (DCM)-water as the crystallization system. DCM acted as a good solvent for racecadotril as well as a bridging liquid for the agglomeration of the crystallized drug and water as the nonsolvent. The prepared agglomerates were tested for micromeritic and mechanical properties. RESULTS: The process yielded ~90 to 96% wt/ wt spherical agglomerates containing racecadotril with the diameter between 299 and 521 µ. A higher rotational speed of crystallization system reduces the size of the agglomerates and disturbs the sphericity. Spherical agglomerates were generated with a uniform dispersion of the crystallized drug. CCA showed excellent flowability and crushing strength. CONCLUSION: Excipients and processing conditions can play a key role in preparing spherical agglomerates of racecadotril by CCA, an excellent alternative to the wet granulation process to prepare intermediates for direct compression.

Solubility of aceclofenac in polyamidoamine dendrimer solutions.

In the present study we investigated the effect of polyamidoamine (PAMAM) dendrimers on the aqueous solubility of aceclofenac. The aqueous solubility of aceclofenac was measured in the presence of dendrimers in distilled water. The effect of variables, such as pH condition, concentration, temperature and generation (molecule size) of dendrimer, has been investigated. Results showed that the solubility of aceclofenac in the dendrimer solutions was proportional to dendrimer concentration. The order in which the dendrimers increased the solubility at a constant pH condition was G3 > G0. The influence of dendrimer solution pH on the solubility enhancement of aceclofenac suggests that it involves an electrostatic interaction between the carboxyl group of the aceclofenac molecule and the amine groups of the dendrimer molecule. The solubility of aceclofenac was inversely proportional to the temperature of dendrimer solution.Different generation (G0 and G3) PAMAM dendrimers have the potential to significantly enhance the solubility of poor water-soluble drugs.

Prefilled syringes: An innovation in parenteral packaging.

Parenteral administration of pharmaceutical products is one of the most popular methods used to produce quick onset of action and also 100% bioavailability. Main problem occurs with the parenteral drug delivery is lack of convenience, affordability, accuracy, sterility, safety etc. Such drawbacks with this delivery system makes it less preferable. Hence, all the disadvantages of these systems can be easily overcome by use of prefilled syringes. The objective of this review article is to provide information regarding prefilled syringes; it's method of preparation, direction to use, advantages, its future scope, and development.

Formulation and evaluation of fast dissolving tablets of cinnarizine using superdisintegrant blends and subliming material.

The aim of this investigation was to develop fast dissolving tablet of cinnarizine. A combination of super disintegrants, i.e., sodium starch glycolate (SSG) and crosscarmellose sodium (CCS) were used along with camphor as a subliming material. An optimized concentration of camphor was added to aid the porosity of the tablet. A 3(2) full factorial design was applied to investigate the combined effect of two formulation variables: Amount of SSG and CCS. Infrared (IR) spectroscopy was performed to identify the physicochemical interaction between drug and polymer. IR spectroscopy showed that there is no interaction of drug with polymer. In the present study, direct compression was used to prepare the tablets. The powder mixtures were compressed into tablet using flat face multi punch tablet machine. Camphor was sublimed from the tablet by exposing the tablet to vacuum drier at 60°C for 12 hours. All the formulations were evaluated for their characteristics such as average weight, hardness, wetting time, friability, content uniformity, dispersion time (DT), and dissolution rate. An optimized tablet formulation (F 9) was found to have good hardness of 3.30 ± 0.10 kg/cm(2), wetting time of 42.33 ± 4.04 seconds, DT of 34.67 ± 1.53 seconds, and cumulative drug release of not less than 99% in 16 minutes.