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Development of a biodegradable nanoplatform poly(lactic-co-glycolic acid) (PLGA) for co-delivery of two drugs is hugely imperative and beneficial in anticancer therapeutics. In this study, co-deliv...

Anemia is the most common hematological abnormality of chemotherapy, which is responsible for poor clinical outcomes. To overcome this complication, the present study was aimed for developing a Eudragit/polylactic-co-glycolic acid (PLGA) based nanoparticulate system for a model drug paclitaxel (PTX). The study was planned using a simplex lattice mixture design. PTX nanoparticles (PTXNp) were evaluated in vitro for physicochemical properties, hemolytic effects and cytotoxic effects. Further, the nanoparticles were subjected to in vivo screening using rats for hemocompatibility, pharmacokinetic profile, and biodistribution to the vital organs. The PTXNps were 65.77–214.73 nm in size, showed more than 60% sustained drug release in 360 h and caused less than 8% hemolysis. The parameters like red blood cell count, activated partial thromboplastin time (aPTT), prothrombin time (PT) and C3 complement were similar to the negative control. Cytotoxicity results suggested that all the PTXNp demonstrated drug concentration-dependent cytotoxicity. The in vivo pharmacokinetic study concluded that PTXNp formulations had significantly higher blood AUC (93.194.55–163,071.15 h*ng/mL), longer half-lives (5.80–6.35 h) and extended mean residence times (6.05–8.54 h) in comparison to PTX solution (p

Lower generation PAMAM dendrimers have an immense potential for drug delivery with lower toxicity, but these dendrimers yet need certain basic ameliorations. In this study, the brain delivery potential of the synthesized PAMAM-Lf (lower generation PAMAM and lactoferrin conjugate) loaded with memantine (MEM) was explored and evaluated in vitro and in vivo in the disease-induced mouse model. The developed nanoscaffolds were characterized for size, zeta potential and in vitro release. Increase in the average size from 11.54 ± 0.91 to 131.72 ± 4.73 nm, respectively, was observed for drug-loaded PAMAM (i.e., PAMAM-MEM) and PAMAM-Lf (i.e., MEM-PAMAM-Lf). Release profile of MEM from MEM-PAMAM-Lf was slow and sustained up to 48 h. In vivo biodistribution in the Sprague-Dawley rat model revealed that the brain uptake of MEM-PAMAM-Lf was significantly higher than that of MEM alone. The behavioral response study in the healthy rats did not result in any significant changes. The in vivo study in an AlCl

Presently, nanotechnology appears as a powerful and innovative tool in the medical field. It has various advantages over the conventional drug therapy such as therapeutic specificity, has less side effects, reduces dose of drug, has more precise treatment and can access the inaccessible areas of the body like brain, tumor cells, etc. The human brain is the most complicated part of the body which is highly protected with the blood-brain barrier (BBB) and the other protective measures of the body. The available treatments for brain disorder are highly invasive (parenteral or surgical procedures) in nature or cause high peripheral toxicity (oral administration). Thus, a prominent strategy is needed which can easily approach the brain and offers a more specific treatment. Nanomedicines are effective tools used for the diagnosis and treatment of brain disorders. Key words: Brain, neurodegenerative disorders, nanotechnology, gold nanoparticle, quantum dots.

Herbal antioxidant like curcumin holds great potential to treat neurodegenerative disease like Alzheimer's disease. However, its therapeutic potency is obstructed due to rapid metabolism, poor solubility, GI susceptibility, enzymatic degradation and lower bioavailability. Thus, the present work aimed to design and optimize curcumin-loaded NLC (CNL) with higher drug entrapment, prolonged release and better stability. CNL was prepared by modified melt emulsification method followed by ultrasonication. The formulation was optimized by 3 factor 3 level Box-Behnken design using solid: liquid lipid, surfactant concentration and ultrasonication time as independent variable while particle size, entrapment efficiency and % drug release as dependant variable. The design suggested 3.092 solid:liquid lipid, 2.131% surfactant and 4.757 min ultrasonication fit best to get the optimized formulation. The size of the optimized CNL was noted 124.37 ± 55.81 nm, which is in the acceptable range for brain delivery. SEM results also comply with this size range (near 150 nm) and demonstrated almost spherical and uniform particles with porous and uneven surface structures. PDI, zeta potential, entrapment efficiency and % drug release were observed as 0.201 ± 0.00, − 17.2 ± 2.35 mV, 93.62 ± 0.68% and 92.73 ± 0.06%, respectively. The NLC demonstrated initial burst release with subsequent prolonged release of drug for 48 h. Weibull kinetic equation with 0.9958 R2, minimum AIC and maximum MSC value was found best fit to explain the release behavior. The β exponent and diffusional coefficient (n) indicated combined release mechanism with Fickian diffusion as drug release mechanism. Formulation was also found stable at different storage condition.

The diagnosis and treatment of neurological ailments always remain an utmost challenge for research fraternity due to the presence of BBB. The intranasal route appeared as an attractive and alternative route for brain targeting of therapeutics without the intrusion of BBB and GI exposure. This route directly and effectively delivers the therapeutics to different regions of the brain via olfactory and trigeminal nerve pathways. However, shorter drug retention time and mucociliary clearance curtail the efficiency of the intranasal route. The in situ mucoadhesive gel overthrow the limitations of direct nose-to-brain delivery by not only enhancing nasal residence time but also minimizing the mucociliary clearance and enzymatic degradation. This delivery system further improves the nasal absorption as well as bioavailability of drugs in the brain. The in situ mucoadhesive gel is a controlled and sustained release system that facilitates the absorption of various proteins, peptides and other larger lipophilic and hydrophilic moieties. Owing to multiple benefits, in situ gelling system has been widely explored to target the brain via nasal route. However, very few review works are reported which explains the application of in situ nasal gel for brain delivery of CNS acting moieties. Hence, in this piece of work, we have initially discussed the global statistics of neurological disorders reported by WHO and other reputed organizations, nasal anatomy, mechanism and challenges of nose-to-brain drug delivery. The work mainly focused on the use of different stimuli-responsive polymers, specifically thermoresponsive, pH-responsive, and ion triggered systems for the development of an effective and controlled dosage form, i.e., in situ nasal gel for brain targeting of bioactives. We have also highlighted the origin, structure, nature and phase transition behavior of the smart polymers found suitable for nasal administration, including poloxamer, chitosan, EHEC, xyloglucan, Carbopol, gellan gum and DGG along with their application in the treatment of neurological disorders. The article is aimed to gather all the information of the past 10 years related to the development and application of stimuli-responsive in situ nasal gel for brain drug delivery.

Psoriasis is a consistently recurring, inflammatory, autoimmune disorder of the skin, affecting about 2-5% of the world population. Abundant therapeutic agents are accessible for the treatment of psoriasis. Nevertheless, none of them are entirely secure and effective to treat the disease without compromising patient compliance. Furthermore, already existing drugs are supposed to restrain the ailment and alleviate the sign and symptoms with no complete cure. However, they focus on restraining the disease and alleviating the symptoms without providing an absolute cure. Therefore there remains a vital challenge, to explore a new drug moiety or delivery system which could safely and effectively manage psoriasis without compromising patient compliance. Furthermore, conventional formulations offer reduced benefit/risk ratio of anti-psoriatic drugs, which limits the use of existing conventional formulations. Novel formulations based on nanocarriers are a promising prospect to overcome the limitation of conventional formulations by offering a reduction in dose, dosing frequency, dose-dependent, side effects with enhanced efficacy. Presently nano-formulations have gained widespread application for effective and safe treatment of psoriasis. The present review primarily focuses on conventional therapeutic strategy and recent advances in lipid-based, polymer-based and metallic nano-formulations of a variety of anti-psoriatic drugs. The practicability of various nanocarrier systems including liposomes, nanostructured lipid carriers, ethosomes, solid lipid nanoparticles, nanocapsules, micelles, dendrimers, gold nanoparticles and silver nanoparticles have been discussed in detail. The review also traces related patents to exemplify the role of various nanoparticles in psoriasis treatment. In a nutshell, nano-formulations remain established as a promising modality for treating psoriasis treatment as they propose better penetration, targeted delivery, enhanced safety, and efficacy.

Diabetes associated oxidative stress and impaired cholinergic neurotransmission causes cognitive deficits. Although phloridzin shows antioxidant- and insulin sensitizing-activities, its ameliorative potential in diabetes-induced memory dysfunction remains unexplored. In the present study, type 2 diabetes (T2D) was induced by streptozotocin (35 mg/kg, intraperitoneal) in rats on ad libitum high-fat diet. Diabetic animals were treated orally with phloridzin (10 and 20 mg/kg) for four weeks. Memory functions were evaluated by passive avoidance test (PAT) and novel object recognition (NOR) test. Brains of rats were subjected to biochemical analysis of glutathione (GSH), brain-derived neurotrophic factor (BDNF), malonaldehyde (MDA) and acetylcholinesterase (AChE). Role of cholinergic system in the effects of phloridzin was evaluated by scopolamine pre-treatment in behavioral studies. While diabetic rats showed a significant decrease in step through latency in PAT, and exploration time and discrimination index in NOR test; a substantial increase in all parameters was observed following phloridzin treatment. Phloridzin reversed abnormal levels of GSH, BDNF, MDA and AChE in the brain of diabetic animals. Moreover, in silico molecular docking study revealed that phloridzin acts as a potent agonist at M1 receptor as compared to acetylcholine. Viewed collectively, reversal of T2D-induced memory impairment by phloridzin might be attributed to upregulation of neurotrophic factors, reduced oxidative stress and increased cholinergic signaling in the brain. Therefore, phloridzin may be a promising molecule in the management of cognitive impairment comorbid with T2D.

In this modern era, with the help of various advanced technologies, medical science has overcome most of the health-related issues successfully. Though, some diseases still remain unresolved due to various physiological barriers. One such condition is Alzheimer; a neurodegenerative disorder characterized by progressive memory impairment, behavioral abnormalities, mood swing and disturbed routine activities of the person suffering from. It is well known to all that the brain is entirely covered by a protective layer commonly known as blood brain barrier (BBB) which is responsible to maintain the homeostasis of brain by restricting the entry of toxic substances, drug molecules, various proteins and peptides, small hydrophilic molecules, large lipophilic substances and so many other peripheral components to protect the brain from any harmful stimuli. This functionally essential structure creates a major hurdle for delivery of any drug into the brain. Still, there are some provisions on BBB which facilitate the entry of useful substances in the brain via specific mechanisms like passive diffusion, receptor-mediated transcytosis, carrier-mediated transcytosis etc. Another important factor for drug transport is the selection of a suitable drug delivery systems like, liposome, which is a novel drug carrier system offering a potential approach to resolving this problem. Its unique phospholipid bilayer structure (similar to physiological membrane) had made it more compatible with the lipoidal layer of BBB and helps the drug to enter the brain. The present review work focused on various surface modifications with functional ligand (like lactoferrin, transferrin etc.) and carrier molecules (such as glutathione, glucose etc.) on the liposomal structure to enhance its brain targeting ability towards the successful treatment of Alzheimer disease.

NLC is a next-generation lipid nanocarrier, which holds many advantages over other colloidal lipid carrier systems like higher drug loading, better and controlled release and enhanced stability. Owing to the unique structural composition, i.e. crystallized solid and liquid lipid blend, it offers excellent biocompatibility and higher permeation across physiological membranes like BBB. Moreover, the surface of NLC can easily be modified with target-specific ligands, proteins, peptides, etc. which makes it a potential candidate for brain targeting of CNS acting drugs. NLC has found various applications for the treatment of various CNS disorders including Alzheimer’s disease, Parkinson’s disease, schizophrenia, epilepsy, migraine, cerebral ischemia, etc. Among these, the application of NLC towards the treatment of AD has been well-explored in the past two decades. In this piece of work, we have discussed the types of NLC, its composition, fabrication techniques, characterization, stability profile and application in the treatment of AD.

Poor aqueous solubility of anticancer drug bortezomib (BTZ) still remains a major challenge in the development of a successful formulation. The dendrimeric platform can provide a better opportunity to deliver BTZ with improved solubility. BTZ encapsulated in PEGylated PAMAM dendrimers (BTZ-PEG-PAMAM) was characterized and evaluated comparatively with encapsulated and conjugated dendritic formulations. The particle size of BTZ-PEG-PAMAM was 188.6 ± 4.17 nm, with entrapment efficiency of 78.61 ± 2.91% and drug loading of 39.30 ± 1.98%. The aqueous solubility of BTZ in PAMAM-PEG conjugate was enhanced by 68.11 folds in comparison to pure drug. In vitro drug release profile was found to be sustained up to 72 h. A comparative colorimetric MTT assay against A549 and MCF-7 cancer cells resulted in maximum efficacy from BTZ-PEG-PAMAM with IC50 value 333.14 ± 15.42 and 152.60 ± 24.56 nM, respectively. Significantly higher cellular internalization was observed in FITC tagged BTZ-PEG-PAMAM. In vivo pharmacokinetic study performed on Sprague Dawley rats resulted in 8.63 folds increase in bioavailability for BTZ-PEG-PAMAM than pure drug. Pharmacokinetic parameters of BTZ-PEG-PAMAM were better and improved over BTZ and other dendritic formulations. In conclusion, the prepared formulation of BTZ-PEG-PAMAM has given significant outcome and this strategy may be further explored for better delivery of BTZ in future.

To establish a platform for the possibility of effective and safe delivery of Temozolomide (TMZ) to brain via surface engineered (polyamidoamine) PAMAM dendrimer for the treatment of glioblastoma. The present study aims to investigate the efficacy of PAMAM-chitosan conjugate based TMZ nanoformulation (PCT) against gliomas in vitro as well as in vivo. The prepared nanoconjugated formulation was characterized by 1H NMR, FT-IR spectroscopy and for surface morphological parameters. The reported approach was also designed in such a way to ensure toxicity before in vivo delivery through conducting the hemolytic study. Surface morphology was found as per nanoformulation via size, pdi and zeta potential measurement. PCT was more efficacious in terms of IC50 values compared to pure TMZ against U-251 and T-98G glioma cell lines. The in vivo pharmacokinetic parameters proved sustained release fashion such as half-life (t1/2) of 22.74 h (PCT) rather than15.35 h (TMZ) only. Higher concentration was found in heart than brain in bio-distribution studies. This study exhibits the potential applicability of dendrimer and CS in improving the anticancer activity and delivery of TMZ to brain. The attractive ex vivo cytotoxicity against two glioma cell lines; U-251 and T-98G and phase solubility studies of TMZ revealed remarkable results. In vivo studies of prepared nanoformulation were significant and promising that explored the double concentration of TMZ in brain due to surface functionality of dendrimer. The reported work is novel and non- obvious as none of such approaches using chitosan anchored dendrimer for TMZ delivery has been reported earlier.

Primaquine phosphate (PQ) is mainly used as a radical cure therapy to eradicate relapse of malaria at the liver stage, which is particularly caused by P. falciparum and P. vivax. In the present study, PQ-loaded galactosylated gelatin nanoparticles (Gel–LA–PQ–NPs) were formulated using a one-step desolvation technique. The mean particle size of Gel–LA–PQ–NPs was found to be 93.48 ± 6.36 nm with a zeta potential of 4.80 ± 0.20 mV having 69.90 ± 1.53% encapsulation efficiency. Electron microscopy demonstrated that the NPs were spherical in shape and uniformly distributed without any cluster formation. The in vitro release of PQ from Gel–LA–PQ–NPs has been facilitated in sustained manner, and the release was three times slower than the naive drug. The prepared nanoparticles (Gel–LA–PQ–NPs) were significantly (p < 0.0001) less hemolytic than the pure drug PQ. The hematological ex vivo study further supported that the developed Gel–LA–PQ–NPs were safer than PQ. The in vitro antiplasmodium assay revealed that th...

The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy. Herbal bioenhancers play a crucial role in enhancing the bioavailability and bioefficacy of different classes of drugs, such as antihypertensives, anticancer, antiviral, antitubercular and antifungal drugs at low doses. This paper highlights various natural compounds that can be utilized as an efficient bioenhancer. Several herbal compounds including piperine, quercetin, genistein, naringin, sinomenine, curcumin, and glycyrrhizin have demonstrated capability to improve the pharmacokinetic parameters of several potent API. This article also focuses on various United States patents on herbal bioenhancers, which has proved to be beneficial in improving oral absorption of nutraceuticals like vitamins, minerals, amino acids and certain herbal compounds. The present paper also describes proposed mechanism of action, which mainly includes absorption process, drug metabolism, and action on drug target. The herbal bioenhancers are easily available, safe, free from side effects, minimizes drug toxicity, shortens the duration of treatment, lowers the drug resistance problems and minimizes the cost of treatment. Inspite of the fact that herbal bioenhancers provide an innovative concept for enhancing the bioavailability of several potent drugs, there are numerous bioenhancers of herbal origin that are yet to be explored in several vital areas. These bioenhancers must also be implied to enhance the bioavailability and bioefficacy through routes other than the oral route of drug delivery. There is a vast array of unexploited plants which can be investigated for their drug bioenhancing potency. The toxicity profiles of these herbal bioenhancers must not be overlooked. Researches must be carried out to solve these issues and to deliver a safe and effective dose of drugs to attain desired pharmacological response.

Objectives This study aims to develop novel carrier system incorporating luteolin, a poorly soluble biologically active plant active. Methods We investigated a lipid-based drug delivery system to enhance dissolution and absorption profile of luteolin. Luteolin was complexed with phospholipids, and the preparation was characterized. The formulation was evaluated for physicochemical properties, in-vitro solubility or release studies. In vivo anti-inflammatory action of luteolin and its phospholipid complex was evaluated by using carrageenan and 12-O-tetradecanoylphorbol-13-acetate as inducers. Key findings The prepared luteolin–phospholipid complex (LPC) showed drug loading of about 72.64% with average particle size of 152.6 nm. The Fourier transform infrared spectroscopy and thermal studies confirm formation of complex. The solubility of luteolin as LPC was about 2.5 times higher than the solubility of pure luteolin in water. In the diffusion study, LPC showed 95.12% of drug release at the end of 2 h. Animal studies demonstrated significant differences in response of LPC and luteolin. Conclusion LPC was successfully prepared by optimizing the process parameters. The resultant delivery system improved bioavailability and efficacy of luteolin and in the future may become an efficient tool for administration of luteolin.

Objectives In this study, we have used melphalan (ML) as a model drug, used extensively for the treatment of breast cancer. Due to its remarkable haemolytic activity, clinical application of this drug is limited. Methods We incorporated the two synthesized PEGylated melphalan conjugates, viz. MLPEG 2000 and MLPEG 5000, separately into the medium molecular weight chitosan (CS)-based smart thermoreversible in-situ forming injectable hydrogel. Prepared hydrogels were evaluated for gelation time, rheological behaviour, drug release and stability. Key findings Although PEGylated melphalan shows significant increase in aqueous solubility and decrease in haemolytic activity, it was loaded to hydrogel to improve dose frequency and local effect. Hydrogel comprising CS (3.22%, w/v) and glycerophosphate disodium salt (GP) (16%, w/v) showed consistent gelation time and retard the release of drug without compromising its stability. To underline the role of GP, conjugates were loaded into CS solution with and without the GP. Remarkably, absence of GP results in rapid initial burst with nearly complete drug release within 50 h, while addition of GP exhibited drug release up to 100 h. Conclusions Thus, this study highlighted the role of CS/GP thermoreversible injectable hydrogel for successful loading of PEGylated melphalan.

Several methods and techniques are potentially useful for the preparation of microparticles in the field of controlled drug delivery. The type and the size of the microparticles, the entrapment, release characteristics and stability of drug in microparticles in the formulations are dependent on the method used. One of the most common methods of preparing microparticles is the single emulsion technique. Poorly soluble, lipophilic drugs are successfully retained within the microparticles prepared by this method. However, the encapsulation of highly water soluble compounds including protein and peptides presents formidable challenges to the researchers. The successful encapsulation of such compounds requires high drug loading in the microparticles, prevention of protein and peptide degradation by the encapsulation method involved and predictable release, both rate and extent, of the drug compound from the microparticles. The above mentioned problems can be overcome by using the double emulsion technique, alternatively called as multiple emulsion technique. Aiming to achieve this various techniques have been examined to prepare stable formulations utilizing w/o/w, s/o/w, w/o/o, and s/o/o type double emulsion methods. This article reviews the current state of the art in double emulsion based technologies for the preparation of microparticles including the investigation of various classes of substances that are pharmaceutically and biopharmaceutically active.

Traditional medicines that formed the basis of health care throughout the world since the earliest days of mankind are still widely used and have considerable importance in international trade. Recognition of their clinical, pharmaceutical, and economic value is still growing, although this varies widely between countries and therefore regulation of exploitation and exportation is essential, together with international cooperation and coordination for their conservation so as to ensure their availability for the future. World Health Organization and European Union issued the guidelines defined the basic criteria for the evaluation of quality, safety, and efficacy of herbal medicines with the goal of assisting national regulatory authorities, scientific organizations, and manufacturers in assessing documentation, submissions, and dossiers in respect of such products. Legislative controls in respect of medicinal plants have not evolved around a structured control model. There are different ways in which countries define medicinal plants or herbs or products derived from them. The present review highlights the status of different countries adopted various approaches to licensing, dispensing, manufacturing, and trading to ensure their safety, quality, and efficacy.

The oral route is most preferred one as there is ease of administration and it is a painless approach. This favored route is restricted to those drug molecules that are absorbent over gastric mucosa. One of the promising techniques is SMEDDS. Self-micro emulsifying drug delivery system has gained more attention due to enhanced oral bioavailability enabling a reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug towards specific absorption window in GIT, and protection of drugs from the unreceptive environment in the gut. SMEDDS provide the dissolved drugs form, and also its small size of droplets imparts substantial interfacial area for the absorption of drugs. It can simply get penetrated into the GIT which is the major advantages over another emulsion. The present study is performed for the motivation of the graduates towards publication and research. Hence, we have encouraged the graduates to prepare an informative article on the present subject

The transdermal drug delivery systems (TDDS) are drug delivery system that gives rapid, the immediate therapeutic effect of the drug across the patient's skin and its different layers. They are also called as patches. More than 75% of the drugs, now a day's, are taken orally and are not very much effective. To overcome these problems, the transdermal drug delivery system has been evolved. The advantage of transdermal patches is that they deliver the drugs for better systemic effects at a controlled and a predetermined rate. This drug delivery system also endorses the controlled release of drug medicament into the skin of the patients. The chief aim of this drug delivery system is to deliver the drug contents into the systemic circulation through the permeation of skin at a predetermined rate. This article is an overview of different types of transdermal patches, their various method of preparation as well as their various physicochemical evaluation methods. The present study is performed for the motivation of the graduates towards publication and research. Hence, we have encouraged the graduates to prepare an informative article on the present subject.

Mucoadhesion is commonly defined as the adhesion between two materials, at least one of which is a mucosal surface. Over the past few decades, mucosal drug delivery has received a great deal of attention. Mucoadhesive dosage forms may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for the improved therapeutic outcome. Application of dosage forms to mucosal surfaces may be of benefit to drug molecules not amenable to the oral route, such as those that undergo acid degradation or extensive first-pass metabolism. The mucoadhesive ability of a dosage form is dependent upon a variety of factors, including the nature of the mucosal tissue and the physicochemical properties of the polymeric formulation. The present study is performed for the motivation of the graduates towards publication and research. Hence, we have encouraged the graduates to prepare an informative article on the present subject.

Drug induced hemolysis is a frequent complication associated with chemotherapy. It results from interaction of drug with erythrocyte membrane and leads to cell lysis. In recent past, various approaches were made to reduce drug-induced hemolysis, which includes drug polymer conjugation, drug delivery via colloidal carriers and hydrogels, co-administration of botanical agents and modification in molecular chemistry of drug molecules. The basic concept behind these strategies is to protect the red blood cells from membrane damaging effects of drugs. There are several examples of drug polymer conjugate that either are approved by Food and Drug Administration or are under clinical trial for delivering drugs with reduced toxicities. Likewise, colloidal carriers are also used successfully nowadays for the delivery of various chemotherapeutic agents like gemcitabine and amphotericin B with remarkable decrease in their hemolytic activity. Similarly, co-administration of botanical agents with drugs works as secondary system proving protection and strength to erythrocyte membranes. In addition to the above statement, interaction hindrance between RBC and drug molecule by molecular modification plays an important role in reducing hemolysis. This review predominantly describes the above recent approaches explored to achieve the reduced hemolytic activity of drugs especially chemotherapeutic agents.

Ease of administration and painless approach made oral route the most preferred. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of dissolution rate limited absorption. Failure to attain intended therapeutic effect of the poor water soluble drugs by this route led to development of novel drug delivery systems which will fulfill therapeutic needs with minimum dose. Although many formulation approaches like solid dispersions, complexation, pH modifications and lipid based delivery systems finding increased appliance with the apparent increase in absorption of drug. Among lipid based formulations, self-micro emulsifying formulations (droplet size < 100 nm) are evident to improve the oral bioavailability of hydrophobic drugs primarily due to their efficiency in facilitating solubilization and in presenting the hydrophobic drug in solubilized form whereby dissolution process can be circumvented. Various components that are used to formulate these dosage forms like surfactants and lipids contribute to the overall improvement in oral bioavailability via promoting the lymphatic transport; thereby hepatic first pass metabolism can be surmounted. The present article gives exhaustive information on the formulation design and characterization of SMEDDS by which the bioavailability can be improved. In this review article, the various aspects of pharmaceutical SMEDDS where compiled together and target audience are specifically the B. Pharm and M. Pharm students so that their knowledge towards the subject concern can be enhanced and also at the same time can be motivated towards the publication.

The current article has been focused on the Mucoadhesive drug delivery system may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for improved therapeutic outcome. Mucoadhesion is commonly defined as the adhesion between two materials, at least one of which is a mucosal surface. Application of dosage forms to mucosal surfaces may be of benefit to drug molecules not amenable to the oral route, such as those that undergo acid degradation or extensive first-pass metabolism. The Mucoadhesive ability of a dosage form is dependent upon a variety of factors, including the nature of the mucosal tissue and the physicochemical properties of the polymeric formulation. This review article aims to provide an overview of the various aspects of mucoadhesion, Mucoadhesive materials, factors affecting mucoadhesion, evaluating methods, and finally various Mucoadhesive drug delivery systems (buccal, nasal, ocular, gastro, vaginal, and rectal) based on literatures were reported so far. In this review article, the various aspects of pharmaceutical microemulsion were compiled together and the target audiences are specifically the M. Pharm and B. Pharm students so that their knowledge towards the subject concern can be enhanced and also at the same time can be motivated towards the publication.

Transdermal drug delivery systems (TDDS) are dosage forms involves drug transport to viable epidermal and or dermal tissues of the skin for local therapeutic effect while a main function of drug is transported into the systemic blood circulation. The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug diclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems polymeric systems by the solvent evaporation technique and by using Glycerol as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Diclofenac. To improve characters of transdermal drug delivery system (TDDS) was emerged, which will improve the therapeutic efficacy and safety of drugs by specific sites within the body, thereby reducing both the size and number of doses. The present article reviews the selection of drug candidates and polymers suitable to be formulated as transdermal system, advantages, disadvantages of formulation design and the methods of evaluation. In this review article the various aspects of pharmaceutical transdermal drug delivery system where compiled together and the target audience are specifically the M Pharm and B Pharm students so that their knowledge towards the subject concern can be enhanced and also at the same time can be motivated towards the publications.

Metronidazole is widely used antimicrobial drug against Gram-negative and Gram-positive anaerobic bacteria. Floating drug delivery systems (FDDS) offer a number of applications for drugs having poor bioavailability because of narrow absorption window in the upper part of gastrointestinal tract. It was used for preparing floating dosage forms that are designed to retain in the stomach for a long time and have developed as a drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. In the present study hydroxy propyl methyl cellulose (HPMC) and micro crystalline cellulose (MCC) are used in different concentrations and sodium bicarbonate was used as effervescent agent. Five formulations (F1-F5) were prepared and evaluated for various physicochemical parameters like hardness, friability, floating ability and drug release profiles and were found to be within range. In general, these systems can float in the gastric conditions and control the drug release from the tablets. Formulation was optimized on the basis of different tablet properties and drug release pattern in invitro release profile. In this study it was confirmed that the formulations containing polymer like HPMC K15M and MCC showed better floating properties.

Melphalan, a drug used for the treatment of breast, ovaries and a certain type of cancer in the bone marrow, was conjugated to linear methoxy poly (ethylene glycol) (M-PEG) of 2000 and 5000, Da. An ester linkage between polymer and drug was used in the coupling to yield a polymeric prodrug. Purified esters were characterized by Maldi-Tof and IR spectroscopy methods. The modification allowed overcoming the known melphalan aqueous solubility problem (0.1 µg/ml) leading us to obtain a polymer-drug bioconjugate more suitable for oral and parental administration. It was found that molecular weight of M-PEG is critical for the conjugates stability, aqueous solubility (80 times and 123 times higher aqueous solubility for M-PEG 2000 and M-PEG 5000, respectively), and hemolytic activity. The melphalan caused 100% hemolysis above the concentration 3.5 µg/ml in 1 h. whereas conjugate of M-PEG 2000 and M-PEG 5000 shows 81.3 ± 0.5% and 48.8 ± 1.5% hemolysis, respectively at 32 µg/ml after1 h. Further In vitro anticancer activity of melphalan and its conjugates was performed with breast cancer MCF-7 cell lines. It shows that LD50 concentration was higher 1.14 and 2 µm for M-PEG 2000 and M-PEG 5000, respectively in comparison to pure melphalan (0.74 µm). Above studies revealed improved pharmacokinetics properties upon conjugation.

Over the past several years, great advances have been made on development of novel drug delivery systems (NDDS) for plant actives and extracts. The variety of novel herbal formulations like polymeric nanoparticles, nanocapsules, liposomes, phytosomes, nanoemulsions, microsphere, transferosomes, and ethosomes has been reported using bioactive and plant extracts. The novel formulations are reported to have remarkable advantages over conventional formulations of plant actives and extracts which include enhancement of solubility, bioavailability, protection from toxicity, enhancement of pharmacological activity, enhancement of stability, improved tissue macrophages distribution, sustained delivery, and protection from physical and chemical degradation. The present review highlights the current status of the development of novel herbal formulations and summarizes their method of preparation, type of active ingredients, size, entrapment efficiency, route of administration, biological activity and applications of novel formulations.

Background: Although the formulations of the Unani system of medicine are popular, not much scientific work has been reported so far. The present article is an attempt to establish the scientific basis of one of the popular Unani formulations Safoof-ESana, a polyherbal formulation widely used as a laxative. Methods: Investigations were carried out to study the physicochemical and phytochemical properties of Safoof-E-Sana and its active ingredients. Results and Conclusion: The values of percentage loss on drying, angle of repose, Hausner ratio, and Carr's index of the formulation were calculated as 8.25 ± 0.582, 27.68, 1.23, and 19 respectively, which indicate that the moisture content of the formulation is within the range and depict good flow characteristics. The total ash, acid- nsoluble ash, and water-soluble ash were found to be 19.146 ± 0.237, 2.351 ± 0.223, and 49.216 ± 0.634, respectively; the value of total ash indicates that the inorganic contents of the formulation are below the limits. Alcoholic and aqueous extracts of the formulation and ingredients were prepared and evaluated for phytochemical analysis and extractive values, and the results show that alkaloids of the formulation are more soluble in water than in alcohol and the higher aqueous extractive value (45.784 ± 0.876) of Unani formulation depicts that water is a better solvent of extraction for the formulation than ethanol.

Cancer is the major cause of fatality and the number of new cases is increasing incessantly. Conventional therapies and existing anticancer agents cause serious side effects and expand the patient's lifespan by a few years. There is the need to exploit alternative anticancer agents and novel drug delivery system to deliver these agents to the tumor site for the prevention of cancer. Recently, biologically active compounds isolated from plants used for the management of cancer have been the heart of interest. Capsaicin is a major pungent agent present in the chili peppers that is heavily consumed in the world. Capsaicin has demonstrated effectiveness as an anticancer agent, but a restraining factor is its pungency, extremely low aqueous solubility, and poor oral bioavailability which impede its use as an anticancer agent. Many technologies have been developed and applied to conquer this drawback. We bring to light the benefits of this phytoconstituent for treating different types of cancer. We also discussed some of the delivery approaches that have already made an impact by either delivering a drug to target tissue or increasing its bioavailability by many folds.

Mucoadhesive polymers have recently gained interest among pharmaceutical scientists as a means of improving drug delivery by promoting dosage form residence time and contact time with the mucous membranes. Mucoadhesion occurs between two surfaces, one of which is a mucous membrane and another is drug delivery system. Pharmaceutical aspects of mucoadhesion have been the subject of great interest during recent years because mucoadhesion could be a solution for bioavailability problems that result from a too short length of stay of the pharmaceutical dosage form at the absorption site within the gastro-intestinal tract. It has been a great challenge to the pharmaceutical sciences in order to enhance localised drug delivery or to deliver ‘difficult’ molecules (proteins and oligonucleotides) into the systemic circulation. Mucoadhesive systems remain in close contact with the absorption tissue, the mucous membrane, releasing the drug at the site of action leading to increase in bioavailability (both local and systemic effects). Extending the residence time of a dosage form at a particular site and controlling the release of drug from the dosage form are useful especially for achieving controlled plasma level of the drug as well as improving bioavailability. The present review describes mucoadhesion, mucoadhesive polymers and use of these polymers in designing different types of mucoadhesive drug delivery systems. Key words: Mucoadhesion; Mucoadhesive polymers; Mucoadhesive force; Bioadhesive property. DOI: http://dx.doi.org/10.3329/sjps.v4i1.8878 SJPS 2011; 4(1): 91-95