The present study was aimed to prepare and evaluate curcumin-piperine-loaded microspheres, assess their sustained anti-obesity effects in obese rats, and investigate the enhancement of curcumin bioavailability through piperine. Curcumin microspheres were successfully formulated and characterized for particle size, morphology, flow properties, entrapment efficiency, and stability. FTIR analysis confirmed no significant interaction between drug and polymers, while SEM showed spherical particles with smooth surfaces and sizes ranging from 1.676 to 5.490µm. The microspheres exhibited good flow properties, high yield (44.6–97.4%), and satisfactory entrapment efficiency (46.4–73.3%), with optimal performance at a 1:4 drug-to-polymer ratio. Cross-linked formulations demonstrated reduced swelling and pH-dependent, colon-targeted sustained release, as confirmed by mucoadhesive and release kinetics studies. Pharmacokinetic and biodistribution data showed enhanced bioavailability, delayed T max (8 h), and a six-fold increase in AUC compared to plain curcumin. In-vivo results revealed significant reductions in body weight, BMI, lipid parameters (TC, TGs, LDL), glucose levels, and organ weight, with an increase in HDL levels, particularly at the 200mg/kg dose. Stability studies over three months confirmed the robustness of the formulation, making curcumin-loaded microspheres a promising candidate for effective anti-obesity therapy with enhanced bioavailability.
Skin cancer is one of the most deadly forms of cancer, and mortality and morbidity rates are continuously rising. Currently, chemotherapy is one of the most promising option; however, it also suffered various drawbacks. Nanomedicine plays a significant role in the effective treatment of skin cancer because of its powerful anticarcinogenic effect and the advantages of administering drugs only to tumor sites, which enhance therapeutic effectiveness, reduce toxicity, and prevent spreading of tumors. The optimum selection of nanocarriers for the best drugs is the key to efficient therapy as compared to conventional therapy. Moreover, a newer approach to nanotechnology may be used for diagnostic purposes and also improve the survival rate of patients suffering from skin cancer, thus reducing health burden on medical facilities.
There are many different forms of wounds, each with its own set of healing requirements. As a result of this, a plethora of wound dressings have been developed, with their individual sets of qualities. Wound dressings previously consisted mainly of biopolymers, which included honey pastes, plant fibers, and animal fat. It's impractical to expect a single bandage to have all the features necessary to meet all wound-healing needs. However, if a dressing closely adheres to the wound and patient parameters in a "one size fits all" approach, it should try to meet the most ideal requirements. A practical wound dressing should allow the wound to heal in the quickest period and for the least amount of money possible. The need for an appropriate substance to prevent infection and heal the wound with minimal side effects is also important. In recent years, reducing infection, hydrating the wound, stimulating healing mechanisms, hastening wound closure, and reducing scar formation through novel approaches have all been explored to treat impaired and difficult-to-heal wounds. This chapter focuses on novel techniques for wound infection, healing, and prevention based on nanomaterials, such as nanocomposites, nanoparticles, liposomes, and hydrogels. This chapter also discusses different types of polymeric materials that are therapeutically utilized in wound dressings, as well as the events that occur at the cellular level that promote the healing process.
Recently, coating industries are focusing on more environmentally friendly coating materials with the help of various uses of oils and fats. Paint, varnish, lacquer, enamel, synthetic resins, oilcloth, linoleum, printing ink, insulation, and waterproofing are all products of the coating industry. Various vegetable oils including polymeric constituents such as polyols, alkyds, polyetheramides, polyetheramides, epoxies and polyurethanes are the ultimate materials as protective coatings along with them constitute the single, largest, easily available, low cost, non-toxic, non-depletable, biodegradable. The paint and varnish sector consumed 17% of all non-edible fat. Linseed oil is still used more than any other oil. Large-scale joint studies of raw materials and their applications have been conducted, and this has encouraged knowledge sharing. Linseed oil has now been blended with different oils, and synthetic resins and cellulose derivatives have been used to create a wide range of novel and useful coatings. This chapter provides an overview of recent advancements and future prospects in the use of oils and fats in coatings technology.
Food nanotechnology for its significant interest has recently been generated by packaging. With its wide range of interesting potential uses in the food business, it is rising quickly. Nanotechnology helps in designing functional and bioactive materials, and innovative methods; including instruments for food packaging. It involves production and characterization with manipulation and proper use of any nano-size material with a size range of 1–100 nm. New and innovative materials for food packaging have greatly influenced and benefited the food industry where it retains food quality; improves shelf life with ease storage, transportation, and traceability. This chapter focuses on the traditional and intelligent packaging (IP) of food products with the aid of nanoparticles for active packaging and the difficulties active food packaging is currently facing from artificial nanoparticles.
Proteins and peptides play a vital role in normal cell functioning and maintaining human physiology. Nowadays, many protein therapeutics have been discovered through the advancement of gene technology and recombinant modification at a large scale. Many of them have better therapeutic outcomes when administered by parenteral routes. However, due to the nature and structure of many proteins, therapeutics have suffered from low oral bioavailability such as acid and enzymatic degradation. Oral, buccal, intranasal, pulmonary, transdermal, ophthalmic, and rectal delivery systems are some of the other delivery methods that have been tested for protein delivery with varied degrees of effectiveness. Many researchers have focused on the oral delivery of protein molecules by coating or entrapping within the matrix of polymer. Recently, oral protein and peptide delivery systems based on hydrocolloids such as chitosan, gelatin, and polylactic acid and their copolymers agar, carrageenan, myrrh, etc. have attracted increased attention. In this chapter, we have focus on the delivery of protein and peptides through various novel carriers based on agar, carrageenan, alginate, and myrrh.
Treatment of skin ailments through systemic administration is limited due to toxicity and patients discomfort. Hence, lower risk of systemic side effects from topical dosage forms like ointments, creams, emulsions and gels is more preferred for the treatment of skin disease. Application of lipid based carriers in drug delivery in topical formulations has recently become one of the major approaches to improve drug permeation, safety, and effectiveness. These delivery systems include liposomes, ethosomes, transfersomes, Nanoemulsions (NEs), Solid Lipid Nanoparticles (SLNs) Nanostructured Lipid Carriers (NLCs) and micelles. Most of the liposomes and SLNs based products are in the market while some are under investigation. Transcutaneous delivery of therapeutics to the skin layer by novel lipid based carriers has enhanced topical therapy for the treatment of skin ailments. This article covers an overview of the lipid-based carriers for topical uses to alleviate skin diseases.
Cytarabine is a pyrimidine nucleoside analog used predominantly for acute myeloid leukemia (AML) and also for other indications, including acute lymphocytic leukemia, chronic myelogenous leukemia, and lymphoma by parenteral route due to its low oral bioavailability. Parenteral administration requires constant plasma level, monitoring for its fluctuation and poor patients compliances. Hence the objective of this work is to construct optimized nanosized malleable liposomes of cytarabine to accentuate transdermal delivery of drug to circumvent previously mentioned drawbacks. We also investigated its characteristics and therapeutic efficiency and attempted to systematically explore the penetration enhancing property. Well characterized ethanolic liposomes were also biologically tested for dermatological safety and systemic bioavailability. Ethanolic liposomes were found to be spherical having nanometric size with low polydispersity and high encapsulation efficiency. Skin permeation and deposition studies revealed significant enhancement. In vivo, skin irritation study of developed formulation showed no erythema or scaling vis-à-vis the liposomes. Blood profile of this novel formulation indicated lower lag time with the high amount of drug within 3-12 h after transdermal administration demonstrating the enhanced percutaneous penetration of cytarabine with no erythema, thus leading to patient's compliance by alternative delivery of drug for the treatment of leukemia.
In the present investigation we have prepared and characterized curcumin (CN)-containing chitosan nanoparticles (CS-NPs) coated with Eudragit FS 30D for colon-specific drug delivery for treatment of ulcerative colitis. Methods: CS-NPs were prepared by ionic gelation using tripolyphosphate. To specify pH sensitive delivery, CS-CN-NPs were coated with Eudragit FS 30D by using a solvent evaporation method. Different process parameters were evaluated, and the optimized formulation was characterized by particle size, size distribution, zeta potential and encapsulation efficiency before lyophilization. The lyophilized product was further subjected to Fourier-transform infrared spectroscopy, and particle morphology and in vitro drug release in different media were studied. Results: the kinetics of in vitro drug release from the CS-CN-NPs revealed sustained release behaviour of the developed carriers. In vivo biodistribution study by gamma-scintigraphy showed good accumulation of the developed nanocarriers in the colonic region. Conclusion: sustained and pH stimulated delivery of CN to the colon was successfully attained via coating of CS-NPs with Eudragit FS 30D to circumvent poor absorption and availability of CN.
Colorectal cancer (CRC) is the third most common cancer in men and the second in women worldwide. In colorectal cancer therapy, as it is in other cancers, biodistribution to tumor tissue can be limited and not reach effective concentrations. Concanavalin (Con-A) conjugated polylactic-co-glycolic acid (PLGA) nanoparticles loaded with 5-fluorouracil (5-FU), were prepared and evaluated under in vitro and in vivo conditions. Con-A conjugated 5-FU nanoparticles (CFUNP) was employed as the carriers for cancer treatment. Solvent evaporation method was employed for the preparation of nanoparticles and characterized for particles size, size distribution, zeta potential, surface morphology, % drug entrapment and in vitro drug release in the simulated intestinal fluid. Optimized nanoparticles were conjugated with Con-A and further characterized by Con-A conjugation efficiency, mucoadhesion, and gamma scintigraphy study. Conjugated nanoparticles sustained the drug release significantly (p<0.05) over a period of 24 h when compared to the marketed formulation of 5-FU. A measurable number of counts of 99mTc-tagged CFUNP3 formulation after 24h study period suggested retention of nanoparticles for a prolonged period of time in the colonic region. These results suggested that Con-A conjugated nanoparticles could be considered as a promising carrier for selectively targeting drug(s) to the colon for the treatment of colon cancer.
The present investigation reports the fabrication, optimization and characterization of tristearin based cytarabine solid lipid nanoparticles (SLN). Higher sensitivity of the cytarabine SLN than drug solution on cell line demonstrated the potential of this developed carrier.
Background: Conventional ophthalmic formulations do not contribute to optimal therapy for local fungal infection in the eye. The present work is focus on the targeting ability of Eudragit nanoparticles (NPs) as a novel carrier for enhancing the delivery of antifungal agent to the eye. Methods: Fluconazole loaded Eudragit nanoparticles were prepared from Eudragit RS 100 and RL 100 via solvent displacement technique. Prepared NPs were characterized for particle size and zeta potential, morphology, thermal behavior, viscosity and entrapment efficiency. Results: Developed NPs had a nanometric size (152-210 nm) and a zeta potential of 18-40 mV. In vitro release studies exposed that upto 60% and 70% drug released from RS 100 and RL 100 NPs, respectively within 24 hours. Ocular tolerability test showed that the eye drops of the NPs produced negligible irritation on rabbit eyes. Antifungal efficacy revealed that prepared fluconazole NPs reduced, keratitis as evident by decline in conjunctival hyperemia and hypopyon compared to drug solution. Conclusion: After 90 days of stability study, results were unchanged, indicating the good potential for ocular delivery. From these results we can conclude that fluconazole NPs may represent an efficacious vehicle to deliver the drug into the eye. Keywords: Conjunctival hyperemia, eudragit, fluconazole, nanoparticles, ocular delivery, ophthalmic formulations.
Leukemia is the common cause of death and worldwide incidence of this disease is increasing. Chemotherapy is the first choice for leukemia treatment, but the major limitations of standard therapy are its side effects and poor patient compliances. Therefore it is imperative to look for a therapeutic system with lesser side effects urgently to address the underlying causes of poor treatment outcomes. In such a scenario transdermal route for delivery of chemotherapeutic drugs could be a better alternative to provide sustained drug level, enhanced activity, self administration and better patient compliances. The present work is focus on the design of nanolipid based transdermal carrier, deformable liposomes bearing cytarabine as a model drug for effective delivery of drug with enhanced transdermal flux. Developed nanocarriers were characterized for their size, morphology, entrapment efficiency, skin penetration and irritation. It could be concluded that nanodeformable liposomes accentuated transdermal flux of cytarabine and could provide a new strategy for leukemia.
Anticancer therapies mostly depend on the ability of the bioactives to reach their designated cellular and subcellular target sites, while minimizing accumulation and side effects at non specific sites. The development of nanotechnology based drug delivery systems that are able to modify the biodistribution, tissue uptake and pharmacokinetics of therapeutic agents is considered of great importance in biomedical research and treatment therapy. Controlled releases from nanocarriers can significantly enhance the therapeutic effect of a drug. Nanotechnology has the potential to revolutionize in cancer diagnosis and therapy. Targeted nano medicines either marketed or under development, are designed for the treatment of various types of cancer. Nanocarriers are able to reduce cytotoxic effect of the active anticancer drugs by increasing cancer cell targeting in comparison to conventional formulations. The newly developed nano devices such as quantum dots, liposomes, nanotubes, nanoparticles, micelles, gold nanoparticles, carbon nanotubes and solid lipid nanoparticles are the most promising applications for various cancer treatments. This review is focused on currently available information regarding pharmaceutical nanocarriers for cancer therapy and imaging.
The aim of the present study was to develop solid lipid nanoparticles (SLN) and formulate a hydrogel for enhanced topical delivery of aceclofenac (ACF). The SLN were prepared by the ultrasonic emulsification method and optimized on the basis of stirring speed and lipid content. The optimized formulation was characterized for particle size (189 ± 9.2 nm), polydispersity index (PDI) (0.162 ± 0.02), zeta potential (-32.51 ± 0.12 mV), entrapment efficiency (86.51 ± 2.46%), surface morphology, differential scanning calorimetry (DSC) and X-ray diffraction (XRD). In vivo performance of ACF-loaded SLN hydrogel showed prolonged inhibition of edema, as compared to that observed using plain ACF hydrogel, after 24 h. The results demonstrated that the ACF-SLN formulation for skin targeting could be a promising carrier for topical delivery of ACF.