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1.
Curr Cancer Drug Targets ; 23(8): 620-633, 2023.
Article in English | MEDLINE | ID: mdl-36843367

ABSTRACT

Pancreatic ductal adenocarcinoma (PDAC) is one of the foremost causes of cancer-related morbidities worldwide. Novel nanotechnology-backed drug delivery stratagems, including molecular targeting of the chemotherapeutic payload, have been considered. However, no quantum leap in the gross survival rate of patients with PDAC has been realized. One of the predominant causes behind this is tumor desmoplasia, a dense and heterogenous stromal extracellular matrix of the tumor, aptly termed tumor microenvironment (TME). It plays a pivotal role in the tumor pathogenesis of PDAC as it occupies most of the tumor mass, making PDAC one of the most stromal-rich cancers. The complex crosstalk between the tumor and dynamic components of the TME impacts tumor progression and poses a potential barrier to drug delivery. Understanding and deciphering the complex cascade of tumorstromal interactions are the need of the hour so that we can develop neoteric nano-carriers to disrupt the stroma and target the tumor. Nanodiamonds (NDs), due to their unique surface characteristics, have emerged as a promising nano delivery system in various pre-clinical cancer models and have the potential to deliver the chemotherapeutic payload by moving beyond the dynamic tumor-stromal barrier. It can be the next revolution in nanoparticle-mediated pancreatic cancer targeting.


Subject(s)
Carcinoma, Pancreatic Ductal , Nanodiamonds , Pancreatic Neoplasms , Humans , Nanodiamonds/therapeutic use , Molecular Targeted Therapy , Pancreatic Neoplasms/drug therapy , Pancreatic Neoplasms/pathology , Carcinoma, Pancreatic Ductal/drug therapy , Carcinoma, Pancreatic Ductal/pathology , Tumor Microenvironment , Pancreatic Neoplasms
2.
J Environ Manage ; 330: 117121, 2023 Mar 15.
Article in English | MEDLINE | ID: mdl-36586369

ABSTRACT

Developing an efficient photobioreactor (PBR) and reducing freshwater dependence are among the significant challenges for generating 3rd generation biomass feedstock. Addressing these, the present study focused on developing a modified airlift (MoAL) PBR. Its performance was further evaluated and compared with the traditional airlift PBR by cultivating microalgae in dark fermentation spent wash. Lower mixing time and higher interfacial mass transfer coefficient was observed in the MoAL PBR having a perforated draft tube. Experimentally, the MoAL exhibited the maximum biomass concentration of 3.18 g L-1, which was 30% higher than that of the conventional airlift PBR. The semi-continuous operation of the MoAL (with water recycling) achieved the maximum biomass productivity of 0.83 g L-1 d-1, two folds superior to that of batch culture. The comprehensive biomass characterization (proximate, ultimate, and thermochemical) further confirmed its potential for bioenergy application. Considering that, hydrothermal liquefaction of the biomass resulted in a maximum biocrude yield of 31% w/w with a higher heating value (HHV) of 36.6 MJ kg-1. In addition, the biocrude comprised 66.6% w/w lighter fraction (<343 °C), including 21.5% w/w of heavy naphtha, 20.5% w/w of kerosene, and 24.6% w/w of diesel. The results can help develop sustainable technology for simultaneous wastewater remediation and biocrude production.


Subject(s)
Microalgae , Photobioreactors , Biomass , Fermentation , Water , Fresh Water
3.
Pharm Nanotechnol ; 10(4): 268-278, 2022 11 15.
Article in English | MEDLINE | ID: mdl-35946098

ABSTRACT

The eye is a one-of-a-kind sensory organ with intricate anatomy and physiology. It is protected by a variety of barriers, ranging from static barriers to dynamic barriers. Although these barriers are very effective at protecting the eye from exogenous substances and external stress, they are highly compromised by various vision-impairing diseases of both the anterior and the posterior segment of the eye. Due to ocular elimination systems and intricate obstacles that selectively limit drug entry into the eye, effective drug delivery to the posterior segment of the eye (PSE) continues to be a challenge in ophthalmology. Since more than half of the most debilitating eye illnesses are thought to originate in the posterior segment (PS), understanding the physiology and clearance mechanism of the eye could help design improved formulations that could be noninvasive and intended for targeted posterior segment therapeutics. Moreover, the major drawback associated with the conventional drug delivery system to PSE is minimal therapeutic drug concentration in the desired ocular tissue and life-threatening ophthalmic complications. One possible approach that can be implemented to overcome these ocular barriers for efficient ocular therapy, non-invasive and targeted drug action to the posterior tissues is by designing nanomedicines. This review summarizes the recent non-invasive and patient compliant advances in designing nanomedicines targeting PSE. The various routes and pathways of drug administration to the ocular tissue are also summarized.


Subject(s)
Eye Diseases , Humans , Eye Diseases/drug therapy , Eye Diseases/metabolism , Eye/metabolism , Drug Delivery Systems , Nanomedicine , Pharmaceutical Preparations
4.
J Vasc Nurs ; 40(1): 2-10, 2022 Mar.
Article in English | MEDLINE | ID: mdl-35287830

ABSTRACT

BACKGROUND: For Melatonin, the pineal gland hormone, also known as the neuroendocrine hormone, influences angiogenesis by exerting a positive effect on fibroblast, monocyte, and cytokine proliferation. Formulation and study of characteristics of gelation-based Melatonin sponge crosslinked with fructose using the surfactant foaming and freeze-drying method for wound healing application was the objective of our study. The structure of the formulated gelatin sponge was observed using a scanning electron microscope and showed to have abundant and uniform pores. Characteristics were studied using digestibility test, water uptake test, porosity measurement test, moisture uptake test, tensile strength test, folding endurance test, scanning electron microscopy, Fourier transform infrared spectroscopy, and drug entrapment efficiency analysis. RESULTS: The obtained data showed that the formulated sponge had good mechanical properties, water uptake, and water retention capacities. In animal experiments, histological and macroscopic observations showed that wounds covered by gelatin loaded with a Melatonin sponge healed quickly. CONCLUSION: The formulated sponge was a potential wound healing material having suitable physical, mechanical properties and biocompatibility. The graphical abstract is shown in Figure 1.


Subject(s)
Gelatin , Melatonin , Animals , Bandages , Biocompatible Materials/chemistry , Gelatin/chemistry , Humans , Melatonin/pharmacology , Water
5.
Adv Pharm Bull ; 11(4): 651-662, 2021 Sep.
Article in English | MEDLINE | ID: mdl-34888212

ABSTRACT

Purpose: The present study focuses on a systemic approach to develop liposomal aztreonam as a promising dosage form for inhalation therapy in the treatment of pneumonia and explores the in-vitro antimicrobial and cell uptake efficacy. Methods: Liposomes were prepared by ethanol injection method using the lipids - soya phosphatidylcholine (SP) and cholesterol (CH). A central composite design (CCD) was employed to optimize the lipid composition to evaluate the effect on vesicle size, zeta potential and entrapment efficiency of the formulation. A numerical and graphical optimization was carried out to predict the optimized blend. The optimized formulation was characterized for vesicle size, surface charge, encapsulation, surface morphology, differential scanning calorimetry (DSC), powder X Ray Diffraction (PXRD), thermogravimetric analysis (TGA), in vitro diffusion, accelerated stability studies, antimicrobial studies on Pseudomonas aeruginosa NCIM 2200 and in vitro cell uptake studies. Results: The optimized formulation was found to have a particle size of 144 nm, a surface charge of -35 mV, with satisfactory drug entrapment. The surface morphology study proved the formation of nanosized vesicles. The drug release from liposomal matrix was biphasic in nature. The solid-state study revealed the reason for good encapsulation of drug. The moisture retention capacity was found to be minimum. The anti-microbial study revealed the potential antibacterial activity of the optimized formulation over the pure drug. The formulation was found to be safe on the epithelial cells and showed a marked increase in cellular uptake of aztreonam in a lipid carrier. Conclusion: It can be concluded that the optimized liposomal aztreonam could be considered as a promising approach for the delivery of aztreonam through inhalation.

6.
J Food Sci Technol ; 57(4): 1205-1215, 2020 Apr.
Article in English | MEDLINE | ID: mdl-32180617

ABSTRACT

Grapes are one of the most highly consumed fruits across the world. In ancient Europe the leaves and the sap of grape plants has been used in traditional treatment for ages. Besides being a wellspring for vitamins and fibre, the skin and seeds of grapes are highly rich in Polyphenols specifically proanthocyanidins, which can be used as a functional ingredient to address various health issues by boosting the natural bio-processes of the body. Since, grape seeds are by product of wine making companies therefore can be easily procured. The present review article briefly describes the various pharmacological activities of grape seed extract and different experimental studies were done which supports the beneficial health qualities of the extract. Through different and various studies, it was proved that the proanthocyanidin rich grape seed extract provides benefits against many diseases i.e. inflammation, cardiovascular disease, hypertension, diabetes, cancer, peptic ulcer, microbial infections, etc. Therefore, beside from using it as a nutraceutical or cosmeceutical, as a result they may have a potential to substitute or complement in currently used drugs in the treatment of diseases by developing it into other successful pharmaceutical formulations for better future prospective.

7.
Crit Rev Ther Drug Carrier Syst ; 37(6): 511-551, 2020.
Article in English | MEDLINE | ID: mdl-33426832

ABSTRACT

Many of the recently approved drug molecules that are therapeutically successful are found to be incompatible for the development of a novel delivery system and to take part in various health care management. Regardless of having better therapeutic properties, these molecules are barred from their effective clinical uses. The main reason attributed to it is poor solubility and/or poor permeability of drugs which finally emerges the drug to be low bioavailable. Nanoemulsions are one of the most acceptable nanolipoidal drug delivery system and appears to be a hope for the delivery of many of the Biopharmaceutical Classification System (BCS) class II and IV drugs. A nanoemulsion is a thermodynamically unstable isotropic mixture of oil, surfactant, and co-surfactants and is biphasic in nature. It can be either water in oil or oil in water and droplets are found in the range of 5 to 500 nm. The manufacturing and fabrication of nanoemulsions involve various natural, synthetic and semi synthetic materials using either low or high-energy methods. Application of nanoemulsions as a novel drug delivery system through several routes, especially oral, transdermal, ophthalmic, and intranasal, have been increased for various pharmacological aspects such as cardiovascular, anticancer, antimicrobial, and ophthalmic due to their stability, high solubilization capacity, and ease of preparation. The objective of this review is to focus on the aspects of manufacturing, fabrication, application, and some toxicological concerns related to nanoemulsions.


Subject(s)
Drug Carriers/chemistry , Drug Compounding/methods , Emulsions/chemistry , Nanoparticles/chemistry , Chemistry, Pharmaceutical , Oils/chemistry , Polysorbates/chemistry , Solubility , Surface-Active Agents/chemistry , Water/chemistry
8.
BMC Chem ; 13(1): 58, 2019 Dec.
Article in English | MEDLINE | ID: mdl-31384806

ABSTRACT

BACKGROUND: Escalating energy security, burgeoning population and rising costs of fossil fuels have focussed our attention on tapping renewable energy sources. As the utilization of food crops for biofuel production culminates into food vs. fuel dilemma, there is an intensive need for alternatives. Production of biofuels from lignocellulosic biomass owing to its profuse availability and high holocellulose content is a promising area for research. RESULTS: In the present study, pineapple leaf, an agro-industrial waste was pretreated with laccase to enhance the enzymatic digestibility of the substrate for improved production of reducing sugar. Variables determining enzymatic delignification of pineapple leaf waste have been optimized by response surface methodology based on central composite design. Maximum delignification of 78.57%(w/w) resulted in reducing sugar of 492.33 ± 3.1 mg/g in 5.30 h. The structural changes in pineapple leaf waste, after laccase treatment, were studied through Fourier transformed infrared spectroscopy, X-ray diffraction and Scanning electron microscopy. Specific surface area, pore volume, and pore diameter of the substrate were studied using the Brunauer-Emmett-Teller and Barrett-Joyner-Halenda methods and found a significant increase in the aforementioned parameters after delignification. CONCLUSION: Laccase mediated delignification of pineapple leaf waste is a cleaner sustainable process for enhanced production of reducing sugar which can accomplish the demand for biofuels.

9.
Article in English | MEDLINE | ID: mdl-31333141

ABSTRACT

BACKGROUND: In recent decades, enormous efforts for different drug discovery processes have led to a number of drug molecules available today to overcome different challenges of the health care system. Unfortunately, more than half of these drugs are listed in either BCS (biopharmaceutical classification system) class II/ IV or both are eliminated from the development pipeline due to their limited clinical use. A nanotechnological approach bears much hope and lipoidal fabrication is found to be suitable for the delivery of such drugs. Nanoemulsion based gel i.e. nanoemulgel out of different nanolipoidal formulations has been found to be a suitable approach to successful drug delivery through topical routes. In past few years many herbal and synthetic active pharmaceutical ingredients (APIs) has been patented as nano sized emulsified gel for various therapeutic activities. METHODS: Nanoemulgel is basically an emulsion-based topical gel formulation, where nanosized emulsion globules can be prepared with the help of high energy or low energy methods and further converted into nanoemulgel by adding a suitable gelling agent. Nanoemulgel fabrication enlists various kinds of polymeric materials, surfactants and fatty substances of natural, synthetic and semi-synthetic nature with a globule size range from 5 to 500 nm. RESULTS: Nanoemulgel can be applicable to various acute and chronic diseases through topical routes. CONCLUSION: Nanoemulgel preparations of many recently approved drugs are being used successfully in different areas of health care and have re-defined the significance of topical route of delivery as compared to other routes. However, along with various improvements in the current state of the delivery system, the safety factor needs to be taken into account by toxicological studies of the materials used in such formulations.


Subject(s)
Drug Carriers/chemistry , Emulsions/administration & dosage , Emulsions/chemistry , Gels/administration & dosage , Gels/chemistry , Nanoparticles/chemistry , Skin/drug effects , Administration, Topical , Drug Delivery Systems/methods , Humans , Nanotechnology/methods
10.
Eur J Ophthalmol ; 29(1): 113-126, 2019 Jan.
Article in English | MEDLINE | ID: mdl-29756507

ABSTRACT

Delivery of drugs to eyes is a great challenge to researchers because of a number of barriers in the eye preventing the actual dose from reaching the site. A number of ophthalmic delivery systems have been developed in the past couple of years that are not only new but also safe and reliable and help to overcome all those barriers in the eye which are responsible for the very less bioavailability of drugs. In this review, we tried to focus on current research in ocular delivery of drug substances giving special emphasis to liposomal delivery system. A brief analysis of other novel ocular delivery systems, ocular physiology, and microbial sources of disease are also highlighted herein. We analyzed the various research findings for churning a general idea for novel ocular delivery system and its future use. The novel formulations may overcome the addressed problems of ophthalmic medication and comply with the quality assurance issues. The liposomal delivery is advantageous as they have the ability to entrap both hydrophobic and hydrophilic drugs and are suitable for delivery to both the anterior and posterior segment of the eye. Therefore, the use of this alternative approach is quite a necessity.


Subject(s)
Drug Delivery Systems , Eye Diseases/drug therapy , Liposomes , Pharmaceutical Preparations/administration & dosage , Administration, Ophthalmic , Animals , Humans , Hydrophobic and Hydrophilic Interactions , Ophthalmic Solutions/therapeutic use
11.
Curr Drug Deliv ; 16(1): 26-41, 2019.
Article in English | MEDLINE | ID: mdl-30227817

ABSTRACT

Wound infections impose a remarkable clinical challenge that has a considerable influence on morbidity and mortality of patients, influencing the cost of treatment. The unprecedented advancements in molecular biology have come up with new molecular and cellular targets that can be successfully applied to develop smarter therapeutics against diversified categories of wounds such as acute and chronic wounds. However, nanotechnology-based diagnostics and treatments have achieved a new horizon in the arena of wound care due to its ability to deliver a plethora of therapeutics into the target site, and to target the complexity of the normal wound-healing process, cell type specificity, and plethora of regulating molecules as well as pathophysiology of chronic wounds. The emerging concepts of nanobiomaterials such as nanoparticles, nanoemulsion, nanofibrous scaffolds, graphene-based nanocomposites, etc., and nano-sized biomaterials like peptides/proteins, DNA/RNA, oligosaccharides have a vast application in the arena of wound care. Multi-functional, unique nano-wound care formulations have acquired major attention by facilitating the wound healing process. In this review, emphasis has been given to different types of nanomaterials used in external wound healing (chronic cutaneous wound healing); the concepts of basic mechanisms of wound healing process and the promising strategies that can help in the field of wound management.


Subject(s)
Dermatologic Agents/administration & dosage , Drug Carriers/chemistry , Nanostructures/chemistry , Wound Healing/drug effects , Wound Infection/therapy , Administration, Cutaneous , Chronic Disease/epidemiology , Chronic Disease/therapy , Humans , Morbidity , Skin/drug effects , Skin/injuries , Treatment Outcome , Wound Infection/epidemiology
12.
Sci Rep ; 8(1): 14114, 2018 09 20.
Article in English | MEDLINE | ID: mdl-30237586

ABSTRACT

The phenomenon of draining, although ubiquitous in nature, has received scant attention especially in the meso-scale. We observe that closed top tubes drain by the inception of an axisymmetric 'Taylor finger' while a minute pierce of the top closure results in an altogether different physics with air entry from the top pushing the liquid out. Again, a coupled mechanism comprising full bore followed by film draining is observed for "too small" a top pierce at "high enough" Eotvos number. Top pierce initiates draining in dimensions which would not drain otherwise and finger entry hastens the process of draining. The myriad of phenomena thus exhibited is depicted as phase diagrams in vertical and inclined conduits. A mechanistic model has been proposed to predict draining and the onset of finger entry in vertical tubes.

13.
Pharm Nanotechnol ; 5(1): 32-43, 2017.
Article in English | MEDLINE | ID: mdl-28948909

ABSTRACT

BACKGROUND: Lornoxicam, is a NSAID of the oxicam class. Its short duration of action owing to rapid elimination and gastrointestinal side effects limits its usefulness when administered orally. OBJECTIVE: The primary objective of the proposed work is to develop suitable lipid nanocarriers for transdermal delivery of Lornoxicam with increased drug residence time at local site of inflamation and in systemic circulation, overcoming undesired gastrointestinal side effects. METHOD: Lornoxicam loaded lipid nanocarriers like solid lipid nanocarriers (SLN), nano-structured lipid carriers (NLC) & nanoemulsions (NE) were prepared by high-speed homogenization technique. RESULT: The particle size, zeta potential, and polydispersity index as obtained, were in the range of 140- 193 nm, -22 to -32 mV, and 0.354-0.301 for SLN formulations and 146-201 nm, -23 to -30 mV, and 0.355-0.354 for NLC formulations respectively. Characterization of stable NE revealed that globule size, zeta potential and polydispersity index were within the range of 138 to 195 nm, -26.1±0.123 mV and 0.195 ± 1.231 respectively. It was also observed that entrapment efficacy and drug loading improved as the lipid concentration was increased. The results obtained from the in vitro permeation study and in vivo anti-inflammatory study showed controlled drug permeation, increased bioavailability, longer retention and better therapeutic potential of Lornoxicam after transdermal application of lipid nanoparticles as compared to conventional gel. CONCLUSION: It can be concluded that the developed lipid nanoparticle loaded gel was found to be a suitable drug delivery carrier for transdermal delivery of Lornoxicam to increase the residence time of drug in systemic circulation and to combat the gastrointestinal side effects.


Subject(s)
Drug Carriers/chemistry , Lipids/chemistry , Nanoparticles/chemistry , Piroxicam/analogs & derivatives , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Drug Compounding , Emulsions , Female , Humans , Male , Particle Size , Piroxicam/administration & dosage , Piroxicam/chemistry , Rats, Wistar , Skin Absorption , Surface Properties , Viscosity
14.
Int J Pharm ; 529(1-2): 629-641, 2017 Aug 30.
Article in English | MEDLINE | ID: mdl-28723407

ABSTRACT

Lipid-drug conjugates (LDC), which may also be addressed as lipoidal prodrug, have the therapeutic actives chemically bound to a lipid moiety like fatty acids or phospholipids. Fabricated in nano-size, lipid-drug conjugate forms another breed of lipid nanoparticles. LDCs are prepared in order to increase the drug loading and hence prevent leakage of a highly polar drug from a lipophilic matrix. In turn, it assists to achieve active targeting of therapeutics with reduced side effect by altering the pharmacokinetic profile of the drug. These self-assembled systems take the benefit of metabolic pathways of lipid biochemistry, allowing suitable organ targeting depending upon its size. These lipids because of its similarities with physiological lipids, enhances the solubility of the therapeutic agents and thereby improve the bioavailability. This present review is meant to encompass different aspects related to lipid drug conjugates which include types of lipids and drugs that can be used to develop this type of formulation. Here, we throw light on methods of preparation of lipid drug conjugate, processing them into nanoparticle, its characterization and different applications of lipid drug conjugate. We aim to present a holistic view on lipid drug conjugate as a suitable drug delivery approach.


Subject(s)
Drug Carriers/chemistry , Lipids/chemistry , Nanoparticles/chemistry , Biological Availability , Solubility
15.
Indian J Dermatol ; 60(4): 419, 2015.
Article in English | MEDLINE | ID: mdl-26288424

ABSTRACT

BACKGROUND: Vitamin B12 deficiency is thought to be uncommon in the eastern parts of India including Bengal and the eastern states as compared to the northern and southern parts of India. The importance of cutaneous features in relation to vitamin B12 deficiency is not well described in literature. AIM: To know the clinical profile of vitamin B12 deficiency in this region and to find out if there is any relationship between dermatologic manifestations with vitamin B12 deficiency. MATERIALS AND METHODS: All symptomatic patients of anemia requiring blood transfusions who had either raised mean corpuscular volume (MCV) or bicytopenia/pancytopenia on complete blood count or were symptomatic in the form of skin hyperpigmentation were screened for vitamin B12 deficiency. RESULTS: Twenty-five patients were tested for vitamin B12 deficiency. Of them 19 patients were found to be having vitamin B12 deficiency. CONCLUSIONS: Vitamin B12 deficiency is not uncommon in the eastern parts of India, contrasting the previous thoughts that it was uncommon in this area, though larger studies are required to know it better. This study included only those requiring blood transfusions, thus a much higher prevalence is expected in this area. Patients with vitamin B12 deficiency do present with severe anemia requiring blood transfusions and often have skin hyperpigmentation.

16.
Drug Dev Ind Pharm ; 41(7): 1095-9, 2015.
Article in English | MEDLINE | ID: mdl-24980914

ABSTRACT

OBJECTIVE: The main objective of this study is to develop a safer non-invasive treatment for nail infections since the current treatment regimen has drawbacks like, incidence of systemic side-effects and higher cost. Proposed topical treatment on the other hand can drastically improve the situation, hence highly desirable. This work was undertaken with a hypothesis to develop a transungual microemulsion gel for topical treatment of onychomycosis. METHODS: Benzyl alcohol and isopropyl myristate were used as oil, Pluronic F68 as surfactant and ethanol as co surfactant, in double-distilled water and loading itraconazole as the model antifungal drug. Pseudo-ternary phase diagram was developed by titrating different ratios of total oil and water with total surfactant, and Km ratio was fixed at 1:1. Microemulsion formulations were prepared based on the phase diagram and incorporated in gels by adding Carbopol 934P. Nail permeation enhancers like urea and salicylic acid were used to increase drug permeation through the nail plate. Parameters like drug loading, clarity, particle size distribution, drug entrapment efficiency (DEE), drug release profile, release kinetics and nail uptake were checked for the evaluation of the formulations. RESULTS: Complete release of drug from the formulation varied from 60 to 120 min. The optimized formulation had DEE of 92.75%, complete drug release in 60 min and highest nail uptake of 0.386%/mm(2) (39 µg of drug) with 5% urea as nail permeation enhancer. CONCLUSION: The formulation may prove beneficial in safer treatment of onychomycosis.


Subject(s)
Drug Delivery Systems , Itraconazole/administration & dosage , Nails/metabolism , Onychomycosis/drug therapy , Administration, Topical , Antifungal Agents/administration & dosage , Antifungal Agents/adverse effects , Chemistry, Pharmaceutical/methods , Drug Liberation , Emulsions , Excipients/chemistry , Gels , Humans , Itraconazole/adverse effects , Particle Size , Permeability , Surface-Active Agents/chemistry , Urea/chemistry
17.
Curr Drug Deliv ; 11(1): 132-8, 2014.
Article in English | MEDLINE | ID: mdl-24266509

ABSTRACT

The objective of this work was to increase the solubility, in vitro skin permeability of lornoxicam from semisolid topical formulations and also to investigate the in vivo potential of nanoemulsion formulation. Optimized lornoxicam loaded nanoemulsion was prepared successfully by spontaneous self-emulsification method and the size of the stable formulations was found within the range of 102 to 200 nm. The stable nanoemulsion formulations characterized for viscosity, droplet size, transmission electron microscopy (TEM) and refractive index. In vitro permeation rate of nanoemulsion and conventional gel of lornoxicam (LX) were determined. Prmeability parameters like steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio (Er) were significantly increased in nanoemulsion NE8 and the nanogel NG8 as compared to conventional gel (LG). In vivo studies revealed a significant increase in anti-inflammatory effects as compared with conventional gel of LX. The anti-inflammatory effects of formulation NG8 showed a significant increase in percent inhibition value when compared with control, this difference was found to be highly significant (p<0.001). This work shows for the first time that lornoxicam can be formulated into nanoemulsions and may show promise in enhancing solubility and permeation.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Nanoparticles , Piroxicam/analogs & derivatives , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/metabolism , Chemistry, Pharmaceutical , Disease Models, Animal , Edema/chemically induced , Edema/prevention & control , Emulsions , Freund's Adjuvant , Gels , Inflammation/chemically induced , Inflammation/prevention & control , Microscopy, Electron, Transmission , Nanomedicine , Particle Size , Permeability , Piroxicam/administration & dosage , Piroxicam/chemistry , Piroxicam/metabolism , Rats , Rats, Wistar , Skin/metabolism , Skin Absorption , Solubility , Surface-Active Agents/chemistry , Technology, Pharmaceutical/methods , Viscosity
18.
Curr Drug Deliv ; 10(6): 656-66, 2013 Dec.
Article in English | MEDLINE | ID: mdl-24274634

ABSTRACT

Solid lipid nanoparticles (SLN) are very potential formulations for topical delivery of anti-inflammatory and anti-arthritic drugs. The solid state of the lipid particles enable efficient drug encapsulation and controlled drug release. In the present study, the evaluation of different formulation parameters based on variation of concentration of lipid and cosurfactant was studied. The SLN gel formulations of the dispersions were compared to the SLN dispersions and with the marketed gel of aceclofenac. The SLNs were prepared by high speed homogenization and ultra-sonication method with fixed amount of aceclofenac (10%) and pluronic F68 (1.5%). The particle size, zeta potential and span of developed formulations was found to be within the range of 123 nm to 323 nm, -12.4 to -18.5 and 0.42 to 0.86 respectively as the lipid concentration was increased from 7.5% to 40%. The highest entrapment efficiency was found to be 75% with the formulation having lipid concentration of 30% and 0.85% of phospholipon 90G. Permeation rate and controlled release property of xanthan gum loaded SLN gel formulations and SLN dispersion was studied through excised pig skin for 24hr. The drug release of SLN gel formulations was better controlled as compare to SLN dispersions. In vivo anti-inflammatory study showed that action of aceclofenac was enhanced for SLN dispersion and gel formulations. The results indicated the superiority of SLN based formulations for topical delivery of aceclofenac.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Diclofenac/analogs & derivatives , Drug Delivery Systems , Nanoparticles , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Delayed-Action Preparations , Diclofenac/administration & dosage , Diclofenac/pharmacokinetics , Drug Carriers/chemistry , Drug Compounding/methods , Excipients/chemistry , Gels , Lipids/chemistry , Male , Particle Size , Poloxamer/chemistry , Polysaccharides, Bacterial/chemistry , Rats , Rats, Wistar , Skin/metabolism , Skin Absorption , Swine
19.
Sci Pharm ; 80(3): 749-64, 2012.
Article in English | MEDLINE | ID: mdl-23008819

ABSTRACT

The aim of this study was to prepare nanostructured lipid carriers (NLC)-based topical gel of aceclofenac for the treatment of inflammation and allied conditions. Stearic acid as the solid lipid, oleic acid as the liquid lipid, pluronic F68 as the surfactant, and phospholipon 90G as the co-surfactant were used. NLCs were prepared by melt-emulsification, low-temperature solidification, and high-speed homogenization methods. Characterization of the NLC dispersion was carried out through particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and an in vitro release study. The anti-inflammatory effect of the NLC gel was assessed by the rat paw edema technique and compared to marketed aceclofenac gel. The NLC dispersions exhibited d(90%) between 233 nm and 286 nm. All of the NLC showed high entrapment efficiency ranging from 67% to 82%. The particle size of NLC was further confirmed by the SEM study. The result of DSC showed that aceclofenac was dispersed in NLC in an amorphous state. Both the entrapment and release rate were affected by the percentage of oleic acid, but the method of preparation affected only the entrapment efficiency. The nanoparticulate dispersion was suitably gelled and assessed for in vitro permeation. Finally, NLC-based gels were found to possess superior (almost double) the anti-inflammatory activity compared to the marketed product. The anti-inflammatory activity of NLC gel showed a rapid onset of action, as well as a prolonged duration of action as compared with the marketed gel.

20.
J Indian Med Assoc ; 109(2): 74-8, 2011 Feb.
Article in English | MEDLINE | ID: mdl-21888166

ABSTRACT

Musculoskeletal disorders are common in diabetic subjects. The pathophysiology of these disorders in diabetic patients is not obvious. It could be due to connective tissue disorders, glycosylated end products, vasculopathy, neuropathy or combinations. A wide range of musculoskeletal syndromes have been described in association with diabetes, namely diabetic cheiro-arthropathy, adhesive capsulitis of shoulder, carpal tunnel syndrome, Dupuytren's contracture, hyperostosis, osteo-arthritis, hyperuricaemia, etc. This study was undertaken to find out the prevalence of these conditions in diabetes mellitus and to look for any associations with diabetic complications or therapy. A tertiary care centre-based cross-sectional study was carried out among 100 consecutive diabetic patients (WHO criteria) attending medicine department who were enrolled. The study was done at Calcutta National Medical College and Hospital, Kolkata, from March 2008 to February 2009. The diagnoses of the rheumatic conditions were made by unbiased clinical observations on the basis of standardised case definitions or criteria. Limited joint mobility (29%), adhesive capsulitis (18%), and osteo-arthritis of knee (27%) or hand (17%) were the most common rheumatic conditions in diabetics. Trigger finger (flexor tenosynovitis) and carpal tunnel syndrome were also present in 7% and 5% cases of diabetics respectively. Although hyperuricaemia was present in 9%, clinical gout was present in only 4%. There was no clear association of these syndromes with diabetic renal disease or micro-albuminuria. Most of these conditions were noted in chronic long duration diabetic subjects.


Subject(s)
Connective Tissue Diseases/epidemiology , Diabetes Mellitus/epidemiology , Rheumatic Diseases/epidemiology , Bursitis/epidemiology , Comorbidity , Cross-Sectional Studies , Dupuytren Contracture/epidemiology , Hospitalization/statistics & numerical data , Humans , India/epidemiology , Osteoarthritis/epidemiology , Prevalence
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