Chlorzoxazone belongs to BCS class II with prominent diminished solubility. The drug owing to low solubility has a marked poor bioavailaibility as maximum of it is rendered to the metabolism by CYP2E1 enzyme in the liver. The main purpose of the work is to enhance the solubility of the drug through the formulation of solid dispersions. Various methods like Co-grinding, Co-precipitation, Fusion method, and Closed melting method were used to formulate the Solid Dispersions. The Solid Dispersions were characterized for in-vitro drug release for F1(Fusion 1),F2 (Fusion 2) C1 (Closed Melting 1),C2 (Closed Melting 2),Co-P (Co-precipitation),Co-G (Co-grinding). Based on drug release profile and solubility studies the formulation made by the F2(Fusion method) with the drug, polymer ratio (0.5:1.0) was obtained with bestresu;ts among all. The results showed that the dispersions has a negligible interation in transformation from crystalline to amorphous state.

In recent years, many scientists worldwide have focused attention on the promising use of microtechnology- and nanotechnology-mediated platform for biomedical application, by these, carbon nanomaterials having excellent physicochemical properties and ultralightweight is known as carbon nanotubes or buckytubes measured on the nanoscale, emerged as valuable delivery systems. Carbon nanotubes having a beehive-shaped tube are attractive nanostructures. It also serves as multifunctional transporters in biomedical applications due to their extraordinary properties of drug delivery, by manipulating their surfaces. This chapter describes the history, classification and promising applications of multifunctional carbon nanotubes in drug delivery.

The aim of the present work was to formulate simvastatin-loaded PEGylated solid lipid nanoparticles (PEG-SLNs) for prolonging blood circulation. Plain solid lipid nanoparticles (P-SLNs) were prepared by ethanol injection method. Prepared P-SLNs were PEGylated using carbodiimide chemistry by coupling the amine group of bis-amine PEG with the carboxyl group of the phosphatidylcholine present on the surface of previously formed drug-loaded P-SLNs in the presence of 1-ethyl-3(3-dimethylaminopropyl) carbodiimide (EDC). The success of the pegylation of P-SLNs was confirmed by the IR spectra of P-SLNs and PEG-SLNs. The average particle size and zeta potential for P-SLNs and PEG-SLNs were found to be 322.3 ± 3.71 nm; − 32.7 ± 0.15 and 351.6 ± 1.23 nm; − 10.6 ± 0.79, respectively. DSC curves and XRD pattern confirmed the homogenous dispersion of simvastatin and concluding the presence of simvastatin in an amorphous state in both nanoparticle formulations. A biphasic in vitro drug release pattern was found with both the nanoparticles formulations, P-SLNs shows a drug release of 96.02 ± 2.41% within 48 h, while 91.89 ± 1.72% drug was released from PEG-SLNs within 72 h. PEG-SLNs were found to be less hemolytic toxic as compared to P-SLNs. Prepared PEG-SLNs were found to be long-circulating, with low elimination and better serum profiles.

Objective: The present investigation focused on the novel approach using artesunate (AS) loaded mannosylated conjugated multi-walled carbon nanotubes (M-MWCNTs) for site-specific delivery to the brain in the treatment of cerebral malaria (CM). Methods: The raw MWCNTs were purified by selective oxidation method and then exposed to sequential chemical functionalization according to the following steps: carboxylation, acylation, amine modification and finally, D-mannose conjugation. The AS was loaded via the equilibrium dialysis method in the molar ratio 1:3 of various functionalized sonicated MWCNTs. The functionalized MWCNTs were characterized for elemental analysis, FTIR, TEM, zeta potential and percentage drug entrapment efficiency. The in vitro drug release study was performed on AS conjugated purified MWCNTs (AS-P-MWCNT) and AS conjugated M-MWCNTs. Bio-distribution study was performed on albino rat for quantitative measurement of AS in different organs and blood. Results: The TEM images of M-MWCNTs indicated their open tubular nature and AS-M-MWCNTs suggests the entrapment of AS. The percent drug entrapment of AS-M-MWCNT was found to be 80.29±3.4 %. In vitro AS release from AS-M-MWCNTs was found in a controlled manner at pH 7.4. The bio-distribution studies clearly indicate the superiority of the AS-M-MWCNTs, as compared to the plain drug towards increasing the accumulation of AS in brain. Conclusion: The results suggest that AS-M-MWCNTs could be employed as an efficient nano-carrier for antimalarial therapy in cerebral malaria.

Cancer is one of the most important causes of morbidity and mortality all across the world. On an average, every year approximately 238,000 new cases of brain and other central nervous system tumors are diagnosed around the world. Amongst all, tumors of brain account for nearly 85% to 90% of all primary central nervous system (CNS) tumors. Regardless of tremendous scientific efforts to develop newer diagnostic techniques and latest therapy, the management of brain cancer is still a challenge in neuro-oncology. Inadequate concentration of chemotherapeutics at the site of tumor restricts the complete destruction of malignant cells due to the presence of blood brain barrier. Besides, there is a necessity for improvement in tumor imaging for better characterization and visualization of tumor cells for surgical procedure. Nanoparticles offer the advantages upon many of these concerns i.e., diagnosis, capability to target therapeutic agents to the tumor sites and the ability of getting across the blood-brain barrier. Thus utilization of nanoparticles may lead to breakthrough in brain cancer management.

Hydrogels have received considerable attention in recent years as one of the promising novel drug delivery systems and also for their role as scaffolds for cells, owing to their unique potentials. A number of crosslinking methods have been used for development of the hydrogel matrix structures which can be classified in two groups of chemically- and physically-induced crosslinking. Prodrug-based self-assembled hydrogels represent a novel class of active biomaterials, exploited for biomedical applications especially for stimuli responsive drug delivery devices. The prodrug-based self-assembled hydrogels show many advantages such as enhanced drug loading, controlled drug delivery, reduction of burst 89release, and simultaneous delivery of multiple drugs. The performance of hydrogels can be enhanced by bioconjugation approach using proteins and peptides. Micro and nanofabrication techniques have been used to manipulate bioconjugated hydrogels for modulating cellular function and tissue morphogenesis. The aim of this chapter is to introduce a novel kind of biomaterial-molecular hydrogel especially prodrug and bioconjugated hydrogel for biomedical applications.

Hydrogels have received considerable attention in recent years as one of the promising novel drug delivery systems and also for their role as scaffolds for cells, owing to their unique potentials. A number of crosslinking methods have been used for development of the hydrogel matrix structures which can be classified in two groups of chemically-and physically-induced crosslinking. Prodrug-based self-assembled hydrogels represent a novel class of active biomaterials, exploited for biomedical applications especially for stimuli responsive drug delivery devices. The prodrug-based self-assembled hydrogels show many advantages such as enhanced drug loading, controlled drug delivery, reduction of burst release, and simultaneous delivery of multiple drugs. The performance of hydrogels can be enhanced by bioconjugation approach using proteins and peptides. Micro and nanofabrication techniques have been used to manipulate bioconjugated hydrogels for modulating cellular function and tissue morphogenesis. The aim of this chapter is to introduce a novel kind of biomaterial-molecular hydrogel especially prodrug and bioconjugated hydrogel for biomedical applications.

CNTs is a fullerene molecule, described in 1991 by the Japanese Scientist ‘‘Sumio Iijima’’ as tube-shaped of graphitic carbon, can be obtained either single or multi-walled nanotube, having a diameter measuring on the nanometer scale, and generally known as buckytubes. Carbon nanotubes (CNTs) have established much recent interest as new entities for experimental disease diagnosis and treatment because of their unique electronic, mechanical, thermal, spectroscopic, metallic, semiconducting and superconducting electron transport properties. Carbon nanotubes can be acquired in numerous ways, the general techniques are Arc discharge, Laser ablation, and Chemical vapour deposition (CVD). Carbon nanotubes are discussed in this review in terms of characters, history, structures, properties, synthesis, purification, characterization methods, toxicity and applications. Purification of nanotubes includes many techniques: Acid treatment, oxidation, annealing, ultrasonication, cutting, magnetic purification, chromatography techniques. Further functionalization enhanced the water solubility of CNT's and completely transformed their biocompatibility profile. Carbon nanotubes, due to their large surface areas, unique surface properties, and needle-like shape, can deliver a lot of therapeutic agents, including DNA, siRNAs and proteins to the target disease sites. CNTs can be readily excreted through the renal route by means of degradation through myeloperoxidase (MOP) enzyme. As CNTs have attracted the fancy of many scientists worldwide, the work beyond our expectations and their simple mechanism with long lasting life makes it more reliable to use. The unique and unusual properties of these structures make them a unique material with a whole range of promising applications.

Colorectal cancer (CRC) is the third most common cancer diagnosed worldwide in human beings. Surgery, chemotherapy, radiotherapy and targeted therapies are the conventional four approaches which are currently used for the treatment of CRC. The site specific delivery of chemotherapeutics to their site of action would increase effectiveness with reducing side effects. Targeted oral drug delivery systems based on polysaccharides are being investigated to target and deliver chemotherapeutic and chemopreventive agents directly to colon and rectum. Site-specific drug delivery to colon increases its concentration at the target site, and thus requires a lower dose and hence abridged side effects. Some novel therapies are also briefly discussed in article such as receptor (epidermal growth factor receptor, folate receptor, wheat germ agglutinin, VEGF receptor, hyaluronic acid receptor) based targeting therapy; colon targeted proapoptotic anticancer drug delivery system, gene therapy. Even though good treatment options are available for CRC, the ultimate therapeutic approach is to avert the incidence of CRC. It was also found that CRCs could be prevented by diet and nutrition such as calcium, vitamin D, curcumin, quercetin and fish oil supplements. Immunotherapy and vaccination are used nowadays which are showing better results against CRC.

Delonix regia (Bojer ex Hook) Raffin (Fabaceae), also known as flame of forest, is a semi-deciduous tree, distributed throughout Madagascar, India, Africa, and Northern Australia. Various parts of the plant are traditionally used for the treatment of different ailments such as inflammation, rheumatism, bronchitis, diabetes, anemia, fever, gynecological disorders, and pneumonia. The plant possess antioxidant, hepatoprotective, gastroprotective, wound healing, antiarthritic, larvicidal, antimalarial, antiemetic, antibacterial, antifungal, antiinflammatory, analgesic, antidiarrhoeal, antiheamolytic, diuretic, and anthelmintic activities. This review is an up-to-date compilation on its traditional uses in context to phytochemical and pharmacological perspectives.

Context: HIV-1 associated dementia (HAD) is an evolving disease in the category of neurological disorders.Objective: Nifedipine-loaded solid lipid nanoparticles (SLNs) were developed and coated with Tween 80 to facilitate enhanced brain drug delivery for the treatment of HAD.Materials and methods: SLNs were prepared using solvent injection method. Lipids consisted of tristearin, hydrogenated soya phosphatidylcholine (HSPC) (1.5: 1 w/w). Nifedipine was model drug in this study. Tween 80 (0.5% v/v) was taken as key modulator. SLNs were characterized for particle shape, size, zeta potential, entrapment efficiency, in vitro drug release, DNA fragmentation, cytotoxicity potential and in vivo studies.Results: The SLNs (plain and coated) were found to be in nanometric in size (similar to 120 nm) with more than 70% entrapment efficiency. In vitro drug release profile reflected sustained release up to 48 h. Tween 80-coated SLNs showed higher percentage of DNA fragmentation in vitro and enhanced cell viability in sulforhodamine assay (rat cortical cells) as compared to plain drug and uncoated SLNs due to facilitated uptake of SLNs and reversal of P-gp efflux by virtue of Tween 80. Biodistribution study performed on vital organs, i.e. brain, heart, liver, spleen, lungs and kidney showed increased accumulation of Tween 80-coated SLNs in the brain.Discussion and conclusion: Tween 80 enhanced localization of SLNs in the brain as compared to uncoated SLNs. This approach can be employed effectively to transport chemotherapeutics across the BBB for management of HIV-1 associated dementia and other ailments.

Drug delivery through mouth is still the most acceptable route to administer bioactives for the patient. The colon targeted drug delivery has gained increasing attention towards the treatment of colorectal cancer and other colon related disorders i. e., Crohn's disease, ulcerative colitis, irritable bowel syndrome, and spastic colon. The drugs such as cardiovascular and antiasthmatic agents have also been delivered via colon to avoid first pass metabolism or acidic environment of stomach. Colon targeting has also been demonstrated as a potential tool for systemic delivery of protein/peptide drugs due to relatively low proteolytic activities in the colonic environment. The GIT is dwelt by over 500 bacterial species, each having a specific place in the tract and developing variety of enzymes which are being utilized for development of colon-targeted drug delivery systems. There are various strategies presently followed for colon-targeted delivery i. e., prodrugs that become active at the colonic site, drug-eluting system reacting to the pH, microflora-activated drug delivery systems, hydrogels and matrices, and multicoating time-dependent drug delivery systems. The future steering towards colon targeted bioactives delivery would involve the application of specific binding with colonic mucosa.

Skin is the largest and easily accessible organ of the body and therefore can be extensively used as a prominent route of delivery for local and systemic effects. Though it presents a multifunctional barrier between body and surrounding particles, there are chances to deliver therapeutic nanocarrier, particularly in diseased skin. Both for dermal and transdermal drug delivery, the horny layer, i.e., the uppermost layer of the skin serve as the most resistant layer to be crossed and for this purpose, different perforation techniques are used that relatively widen the skin opening and allow the passage of drug (≤ 10 mg) and micromolecules, but this amateur disruption of the skin can be avoided in order to preserve this barrier against cutaneous microbiota by using deformable nanocarriers. In this review, we discuss the nanosized aggregates and microneedle technology for the advanced delivery of vaccines, protein, peptides, nucleic acid, and hormone across the skin.

One of the most significant characteristics of cancer cells is their rapid dividing ability and overexpression of LDL receptors, which offers an opportunity for the selective targeting of these cells. 5-Fluorouracil (5-FU)-encapsulated low density lipid nanoparticles (LDLN) were prepared by the emulsion congealing method which mimics the plasma-derived LDL by acquiring the apolipoprotein B-100 from the blood. The average particle size, transmission electron microscope (TEM), and drug content of the prepared LDLN dispersion were found to be 161±3.5 nm, with spherical shape, and 0.370±0.05 mg/mL, respectively. In vitro release studies revealed a sustained profile which decrea-sed with a lapse of time. In vivo studies of 5-FU serum concentration and biodistribution revealed a 5-FU serum concentration of 8.5% in tumor cells and about 2.1% in the liver at the end of 24 hr from LDLN. Tumor growth suppres-sion studies showed 185.42% average tumor growth and 89.76% tumor height as compared to the control exhibiting tumor growth at 1166.47% and tumor height at 176.07%. On the basis of these collective data, it is suggested that a higher accumulation of LDLN, when given as an IV, in solid tumors is attributed to the active uptake of LDLN via LDL receptors via apolipoprotein B-100.

Pharmaceutical and biotechnological research sorts protein drug delivery systems by importance based on their various therapeutic applications. The effective and potent action of the proteins/peptides makes them the drugs of choice for the treatment of numerous diseases. Major research issues in protein delivery include the stabilization of proteins in delivery devices and the design of appropriate target-specific protein carriers. Many efforts have been made for effective delivery of proteins/peptidal drugs through various routes of administrations for successful therapeutic effects. Nanoparticles made of biodegradable polymers such as poly lactic acid, polycaprolactone, poly(lactic-co-glycolic acid), the poly(fumaric-co-sebacic) anhydride chitosan, and modified chitosan, as well as solid lipids, have shown great potential in the delivery of proteins/peptidal drugs. Moreover, scientists also have used liposomes, PEGylated liposomes, niosomes, and aquasomes, among others, for peptidal drug delivery. They also have developed hydrogels and transdermal drug delivery systems for peptidal drug delivery. A receptor-mediated delivery system is another attractive strategy to overcome the limitation in drug absorption that enables the transcytosis of the protein across the epithelial barrier. Modification such as PEGnology is applied to various proteins and peptides of the desired protein and peptides also increases the circulating life, solubility and stability, pharmacokinetic properties, and antigenicity of protein. This review focuses on various approaches for effective protein/peptidal drug delivery, with special emphasis on insulin delivery.