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1.
Electrophoresis ; 44(7-8): 711-724, 2023 04.
Article in English | MEDLINE | ID: mdl-36720044

ABSTRACT

A number of microfluidic systems of interest essentially consist of micro-scaled channels/tubes, whose walls are inherently rough. The novelty of the current study lies in exploring the impact of the wall roughness on mass transfer in the case of flow through a microtube with porous wall. The current investigation is possibly the first attempt at exploring the effect of mass transfer for a porous-walled, rough microtube, as earlier studies were limited to the analysis of hydrodynamic and thermal effects only in an impervious microtube. In particular, the effects of the corrugation amplitude and the wavenumber on the mass transport have been assessed in detail in this work, via a combination of perturbation approximations and numerical analysis. Several interesting revelations are elicited regarding the effects of these pertinent parameters on the mass transfer coefficient, permeation flux, wall surface concentration, and delivery flux of the neutral solute. It has been unveiled that it is possible to enhance the solute mass flux by 10% via appropriate tuning of corrugation amplitude. The findings of the study can help in better understanding of mass transport for a porous-walled, rough microtube, which has critical relevance in several important applications such as micromixers, targeted drug delivery, and so on.


Subject(s)
Electroosmosis , Models, Theoretical , Porosity , Microfluidics , Solutions
2.
Drug Dev Ind Pharm ; 46(2): 227-235, 2020 Feb.
Article in English | MEDLINE | ID: mdl-31928244

ABSTRACT

Objective: Aim of the present work was to optimize and formulate resveratrol loaded vesicular cream intended for dermal delivery of resveratrol with high skin deposition potential.Methods: Formulation was developed and optimized using Central Composite Design. Amount of phospholipid and sodium cholate were selected as critical material attributes and vesicle size and entrapment efficiency of resveratrol were taken as critical quality attributes. To increase the skin applicability and patient compliance, vesicles were further developed as vesicular cream which was then thoroughly characterized for physicochemical parameters, ex vivo skin permeation/deposition profile and antioxidant potential.Results: Vesicle size and entrapment efficiency of the optimized batch were found to be 178.9 ± 12.87 nm with 72.32 ± 3.45% respectively. Physicochemical properties and viscosity of cream formulation were also found to be favorable for skin applicability. Permeation flux at the end of 24 h was found to be 2.70 ± 0.73, 4.45 ± 0.56 and 4.95 ± 0.69 µg cm-2 h-1 for conventional cream, vesicular dispersion, and vesicular cream formulation respectively. Higher drug deposition in the skin via vesicular cream formulation was observed i.e. 335.2 ± 4.12 µg cm-2 (70.16 ± 0.87%) as compared to conventional cream i.e. 67.12 ± 19.63 µg cm-2 (14.05 ± 4.11%). Resveratrol encapsulated in vesicular cream has retained its inherent antioxidant activity suggesting the stability of resveratrol in vesicular cream.Conclusion: Thus, it can be concluded that deformable vesicular cream is capable of delivering encapsulated bioactive in deeper layers of skin, where it can be retained for achieving higher dermatological benefits.


Subject(s)
Antioxidants/administration & dosage , Antioxidants/chemistry , Ointments/administration & dosage , Ointments/chemistry , Resveratrol/administration & dosage , Resveratrol/chemistry , Skin/drug effects , Administration, Cutaneous , Animals , Chemistry, Pharmaceutical/methods , Drug Carriers/chemistry , Particle Size , Permeability/drug effects , Phospholipids/chemistry , Skin Absorption/drug effects , Swine , Viscosity/drug effects
3.
Int J Mol Sci ; 21(19)2020 Oct 04.
Article in English | MEDLINE | ID: mdl-33020456

ABSTRACT

Fresh and clean water is consistently depleting and becoming a serious problem with rapid increases in population, so seawater desalination technology has captured global attention. For an efficient desalination process, this work proposes a novel, nanofibrous, thin-film composite membrane (NF-TFC) based on the deposition of the nanofibrous active layer of a blend of chitosan (CS) and poly (vinylpyrrolidone) (PVP) crosslinked with maleic acid on a 3-triethoxysilylpropylamine functionalized cellulose acetate substrate. FTIR analysis demonstrated the development of chemical and physical interactions and confirmed the incorporation of functional groups present in the NF-TFC. Scanning electron microscopy (SEM) micrographs depict the fibrous structure of the active layers. The reverse osmosis (RO) desalination characteristics of NF-TFC membranes are elevated by increasing the concentration of the crosslinker in a CS/PVP blend. Cellulose acetate (CA)-S4 attained an optimal salt rejection of 98.3% and permeation flux of 42.9 L/m2h, suggesting that the NF-TFC membranes could be favorable for seawater desalination.


Subject(s)
Chitosan/chemistry , Maleates/chemistry , Nanofibers/chemistry , Water Purification , Filtration , Humans , Osmosis , Seawater/chemistry , Water/chemistry
4.
Recent Adv Drug Deliv Formul ; 18(2): 120-130, 2024.
Article in English | MEDLINE | ID: mdl-38659269

ABSTRACT

BACKGROUND: Crisaborole (CB), a boron-based compound, is the first topical PDE4 inhibitor to be approved by the US Food and Drug Administration (2016) for the treatment of Atopic Dermatitis. It is marketed as a 2% ointment (Eucrisa, Pfizer). However, CB is insoluble in water; therfore, CB glycersomes were formulated to enhance its permeation flux across the skin. OBJECTIVE: We developed a glycerosomal gel of CB and compared its in vitro release and permeation flux with the 2% conventional ointment. METHODS: Glycerosomes were prepared using thin film hydration method employing CB, soya phosphatidylcholine, and cholesterol. The formed film was further hydrated employing a mixture of phosphate buffer pH 7.4 /glycerin solution containing varying percentages (20,30, 40, and 50 %) of glycerol. The glycerosomes obtained were characterized by their size, polydispersity index (PDI), and Zeta potential. The entrapment efficiency of the optimized formulation (F1) was determined. The in vitro release of F1 was compared with its 2% conventional ointment. F1 was further incorporated into carbopol 934 P gel. The gel was characterized by pH, viscosity, spreadability, and drug content. The permeability flux of the glycerosomal gel was compared with its 2% conventional ointment. RESULTS: The optimized CB glycerosomes had a vesicle size of 137.5 ± 50.58 nm, PDI 0.342, and zeta potential -65.4 ± 6.75 mV. CB glycerosomal gel demonstrated a 2.13-fold enhancement in the permeation flux. CONCLUSION: It can thereby be concluded that glycerosomes can be an effective delivery system to enhance the penetration of CB across the skin.


Subject(s)
Boron Compounds , Bridged Bicyclo Compounds, Heterocyclic , Gels , Glycerol , Skin Absorption , Skin Absorption/drug effects , Gels/chemistry , Boron Compounds/chemistry , Boron Compounds/pharmacokinetics , Boron Compounds/administration & dosage , Bridged Bicyclo Compounds, Heterocyclic/pharmacokinetics , Bridged Bicyclo Compounds, Heterocyclic/chemistry , Bridged Bicyclo Compounds, Heterocyclic/administration & dosage , Animals , Glycerol/chemistry , Glycerol/pharmacology , Administration, Cutaneous , Phosphodiesterase 4 Inhibitors/pharmacokinetics , Phosphodiesterase 4 Inhibitors/pharmacology , Phosphodiesterase 4 Inhibitors/administration & dosage , Phosphodiesterase 4 Inhibitors/chemistry , Permeability , Liposomes , Skin/metabolism , Skin/drug effects , Drug Liberation , Ointments
5.
Chemosphere ; 313: 137480, 2023 Feb.
Article in English | MEDLINE | ID: mdl-36513197

ABSTRACT

Forward Osmosis (FO) is a promising separation technology with a wide range of applications in water and wastewater treatment. FO membrane is the core of the forward osmosis process. Recently, the organic membrane has been widely used for forward osmosis applications even though inorganic membrane has excellent mechanical properties, decent chemical resistance, high durability, high porosity, and good hydrophilicity. Nevertheless, the utilization of inorganic membrane is hindered by the heat-intensive steps involved in its fabrication and the use of expensive source material. Geopolymerization provides a cost-effective technique for the preparation of inorganic membranes because of its sintering-free steps and utilization of fly ash as source material. Herein, we present a sintering-free, environmentally friendly, and cost-effective synthesis of geopolymeric membrane for application in forward osmosis. Fly ash was mixed with alkaline activator solution and porous reduced graphene oxide (PRGO) to prepare geopolymer slurry. The hydrogen peroxide and egg albumen were used as foaming agent and surfactant, while the membrane surface was coated with titanium dioxide to enhance the hydrophilicity of the membrane surface. The PRGO content improved the mechanical properties of the geopolymeric membrane. The average maximum flux recorded was 21 L/m2 h with geopolymer substrate having a pore size of 1.8 µm and hydrophilic coated layer pore size of 0.25 µm. The varying concentrations of PRGO control the substrate's mechanical properties and pore size, as well as provide new insights for future studies. These preliminary results show that low-cost geopolymer material is a promising candidate for FO membrane fabrication.


Subject(s)
Coal Ash , Water Purification , Porosity , Osmosis , Membranes, Artificial , Water Purification/methods
6.
Water Res ; 229: 119407, 2023 Feb 01.
Article in English | MEDLINE | ID: mdl-36462260

ABSTRACT

This study provides a comprehensive and systematic overview of the application of gas-liquid two-phase flow with microbubbles in the feed stream to improve heat and mass transfer in direct-contact membrane distillation (DCMD) processes for seawater desalination. A swirl-flow-type microbubble generator (MBG) was installed at the feed-side inlet of the DCMD module to investigate its effect on transmembrane flux. The maximum improvement in the MBG-assisted DCMD permeation flux was found to be approximately 18% at a lower feed temperature (40 °C) and optimal air flow rate (50 cc/min), and an optimal MBG geometry comprising a swirler, a nozzle tip of diameter 2 mm, and a diffuser at an angle of 30°. The results were observed to be related to the number density of microbubbles less than 100 µm in size, which plays an important role in improving heat and mass transfer in two-phase flow. In addition, the simulation results based on conventional heat transfer correlations of bubbly flow underestimated the experimental results. Therefore, this study also aims to propose and verify a new two-phase flow heat transfer correlation. The proposed correlation considers the effects of bubble size distribution to accurately predict the performance of MBG-assisted DCMD processes.


Subject(s)
Microbubbles , Water Purification , Distillation/methods , Membranes, Artificial , Temperature , Water Purification/methods
7.
Membranes (Basel) ; 13(5)2023 May 09.
Article in English | MEDLINE | ID: mdl-37233561

ABSTRACT

Metal-organic framework (MOF) membranes exhibit immense potential for separation applications due to their regular pore channels and scalable pore sizes. However, structuring a flexible and high-quality MOF membrane remains a challenge due to its brittleness, which severely restricts its practical application. This paper presents a simple and effective method in which continuous, uniform, defect-free ZIF-8 film layers of tunable thickness are constructed on the surface of inert microporous polypropylene membranes (MPPM). To provide heterogeneous nucleation sites for ZIF-8 growth, an extensive amount of hydroxyl and amine groups were introduced on the MPPM surface using the dopamine-assisted co-deposition technique. Subsequently, ZIF-8 crystals were grown in-situ on the MPPM surface using the solvothermal method. The resultant ZIF-8/MPPM exhibited a lithium-ion permeation flux of 0.151 mol m-2 h-1 and a high selectivity of Li+/Na+ = 1.93, Li+/Mg2+ = 11.50. Notably, ZIF-8/MPPM has good flexibility, and the lithium-ion permeation flux and selectivity remain unchanged at a bending curvature of 348 m-1. These excellent mechanical characteristics are crucial for the practical applications of MOF membranes.

8.
Saudi Pharm J ; 20(4): 355-63, 2012 Oct.
Article in English | MEDLINE | ID: mdl-23960810

ABSTRACT

The present study deals with the development of transferosomal gel containing insulin by reverse phase evaporation method for painless insulin delivery for use in the treatment of insulin dependent diabetes mellitus. The effect of independent process variables like ratio of lipids (soya lecithin:cholesterol), ratio of lipids and surfactants, and ratio of surfactants (Tween 80:sodium deoxycholate) on the in vitro permeation flux (µg/cm(2)/h) of formulated transferosomal gels containing insulin through porcine ear skin was optimized using 2(3) factorial design. The optimal permeation flux was achieved as 13.50 ± 0.22 µg/cm(2)/h with drug entrapment efficiency of 56.55 ± 0.37% and average vesicle diameter range, 625-815 nm. The in vitro insulin permeation through porcine ear skin from these transferosomal gel followed zero-order kinetics (R (2) = 0.9232-0.9989) over a period of 24 h with case-II transport mechanism. The in vitro skin permeation of insulin from optimized transferosomal gel by iontophoretic influence (with 0.5 mA/cm(2) current supply) also provided further enhancement of permeation flux to 17.60 ± 0.03 µg/cm(2)/h. The in vivo study of optimized transferosomal gel in alloxan-induced diabetic rat has demonstrated prolonged hypoglycemic effect in diabetic rats over 24 h after transdermal administration.

9.
Nanomaterials (Basel) ; 12(18)2022 Sep 06.
Article in English | MEDLINE | ID: mdl-36144881

ABSTRACT

Due to its unique physical and chemical properties, MXene has recently attracted much attention as a promising candidate for wastewater treatment. However, the low water permeation flux of MXene membrane remains a challenge that has not been fully solved. In this study, attapulgite was used to increase the flux of MXene membrane through a facile one-pot method, during which the MXene nanosheets were self-assembled while being intercalated by the attapulgite nanorods to finally form the composite membranes. Under optimal conditions, an increase of water permeation flux of 97.31% could be observed, which was attributed to the broadened nano-channel upon the adequate intercalation of attapulgite nanorods. Its permeation flux and rejection rate for methylene blue (MB) were further studied for diverse applications. In contrast to bare MXene, the permeation flux increased by 61.72% with a still high rejection rate of 90.67%, owing to the size rejection. Overcoming a key technique barrier, this work successfully improved the water permeability of MXene by inserting attapulgite nanorods, heralding the exciting prospects of MXene-based lamellar membrane in dye wastewater treatment.

10.
Gels ; 8(7)2022 Jun 24.
Article in English | MEDLINE | ID: mdl-35877486

ABSTRACT

Chitosan-capped silver nanoparticle (CS-capped AgNPs)-incorporated Poly(vinyl alcohol) (PVA) hybrid membranes were prepared by a solution-casting technique for ethanol dehydration via pervaporation. The incorporation of CS-capped AgNPs into the PVA membrane and its influence on membrane properties and pervaporation-separation process of azeotropic water/ethanol mixture was studied. The addition of CS-capped AgNPs into the PVA membrane reduced the crystallinity, thereby increasing the hydrophilicity and swelling degree of the hybrid membrane, supported by contact angle (CA) analyzer and swelling degree experiments, respectively. Fourier transform infrared spectroscopy (FTIR) demonstrated the formation of polymeric matrix between PVA and CS and also the binding of AgNPs onto the functional group of CS and PVA, which was also reflected in the microstructure images demonstrated by scanning electron microscopy (SEM) and by 2θ angle of wide-angle X-ray diffraction (WAXD). The effect of CS-capped AgNPs on the thermal stability of the hybrid membrane was demonstrated by differential scanning calorimetry (DSC) and thermogravimetric analyzer (TGA). These characteristics of the hybrid membrane positively impact the efficiency of the dehydration of ethanol, as indicated by pervaporation experiments. The best performances in total flux (12.40 ± 0.20 × 10-2 kg/m2 h) and selectivity (3612.33 ± 6.03) at 30 °C were shown for CS-capped AgNPs PVA hybrid membrane containing 2 wt.% CS-capped AgNPs (M-4). This confirms that the developed hybrid membranes can be efficiently used to separate water from azeotropic aqueous ethanol.

11.
J Hazard Mater ; 414: 125489, 2021 07 15.
Article in English | MEDLINE | ID: mdl-33676253

ABSTRACT

It is highly challenging to prepare durable and chemical resistant ultra-permeable membranes that can quickly separate small organic molecules like dye or inorganic salt in the complex textile wastewater industry. Here, side-chain sulfonated poly(ether ether ketone) (SPEEK) was synthesized and prepared the poly(ether ether ketone) (PEEK) - SPEEK nanofiltration (NF) membrane by a simple dipping coating and heat treatment. Single component filtration tests of the optimized membrane showed ultrahigh pure water flux (126 Lm-2 h-1 bar-1) and relatively low NaCl rejection (6.7%). Moreover, the negatively charged membrane exhibited excellent rejection of 98.8% toward Congo red (CR). The pure water flux was about 9 folds than that of commercial NF270 with comparable solutes rejection. The separation tests of CR and NaCl mixed solution at optimized conditions exhibited ultra-high permeation flux (34 Lm-2 h-1 bar-1), satisfactory dye (98.8%)/salt (< 10%) rejection and the separation performance remained stable after 10 cycles. Finally, the contaminated membrane was washed with ethanol, the permeation flux and the CR rejection remained constant after several cycles, while the commercial NF1 membrane exhibited serious swelling only within one cycle. The prepared membrane exhibited good organic solvents resistance and antifouling properties. Thus, this work confirmed the PEEK-SPEEK NF membrane showed great potential in the sustainable treatment of textile wastewater.

12.
J Photochem Photobiol B ; 221: 112246, 2021 Aug.
Article in English | MEDLINE | ID: mdl-34243023

ABSTRACT

Photo-oxidative skin damage is mainly caused by the UV-A radiation of the sun. Synthetic sunscreens used to counter this acts mostly on the superficial skin layer and possess serious side effects. P-coumaric acid (PCA) is a UV-A protective plant phenolic having quick diffusion and distribution in superficial skin layers limiting its application as herbal sunscreen. The present study was designed to formulate an optimized phospholipid complex of PCA (PCAPC) through response surface methodology to enhance its skin permeation to deeper skin layers providing protection against photo-oxidative stress. PCAPC was characterized by FT-IR, DTA, PXRD, TEM, zeta potential etc. PCAPC was then incorporated into a gel formulation (PCAPC-GE) to facilitate its transdermal delivery. Physicochemical properties of the gel were assessed by pH, homogeneity, rheology, spreadability etc. In-vitro SPF and UVA-PF of the gel was evaluated and compared with conventional gel (PCA-GE). Ex-vivo skin permeation flux, permeability coefficient, skin deposition and dermatokinetic analysis were carried out to measure the rate and level of skin permeation. This was accompanied by in-vivo evaluation of PCAPC-GE and PCA-GE in the experimental rat model by measuring the various oxidative stress markers such as superoxide dismutase, catalase etc. PCAPC-GE provided high SPF and UVA-PF value compared to PCA-GE. The physicochemical parameters were suitable for transdermal application. PCAPC-GE enhanced the permeation rate of PCA by almost 6 fold compared to PCA-GE. Besides, a significant reduction of UV-A induced oxidative stress biomarkers were observed for PCAPC-GE. Thus, the PCAPC-GE may be an effective alternative of synthetic sunscreens due to its enhanced permeation and protection against UVA-induced oxidative stress.


Subject(s)
Coumaric Acids/chemistry , Gels/chemistry , Oxidative Stress/drug effects , Phospholipids/chemistry , Protective Agents/pharmacology , Ultraviolet Rays , Animals , Drug Stability , Male , Oxidative Stress/radiation effects , Particle Size , Permeability/drug effects , Permeability/radiation effects , Protective Agents/chemistry , Protective Agents/metabolism , Rats , Rats, Wistar , Rheology , Skin/drug effects , Skin/metabolism , Skin/radiation effects , Solubility , Sun Protection Factor , Transition Temperature
13.
Membranes (Basel) ; 12(1)2021 Dec 31.
Article in English | MEDLINE | ID: mdl-35054583

ABSTRACT

Salts, organic materials, and hazardous materials can be found regularly in the effluent from a desalter unit of crude oil. These materials should be separated from the wastewater. Four kinds of inexpensive and innovative ceramic microfiltration membranes (mullite, mullite-alumina (MA 50%), mullite-alumina-zeolite (MAZ 20%), and mullite-zeolite (MZ 40%)) were synthesized in this research using locally available inexpensive raw materials such as kaolin clay, natural zeolite, and alpha-alumina powders. Analyses carried out on the membranes include XRD, SEM, void fraction, the average diameter of the pores, and the ability to withstand mechanical stress. Effluent from the desalter unit was synthesized in the laboratory using the salts most present in the desalter wastewater (NaCl, MgCl2, and CaCl2) and crude oil. This synthesized wastewater was treated with prepared ceramic membranes. It was discovered that different salt concentrations (0, 5000, 25,000, 50,000, 75,000, and 100,000 mg L-1) affected the permeate flux (PF), oil rejection, and ion rejection by the membrane. Results showed that in a lower concentration of salts (5000 and 25,000 mg L-1), PF of all types of ceramic membranes was increased significantly, while in the higher concentration, PF declined due to polarization concentration and high fouling effects. Oil and ion rejection was increased slightly by increasing salt dosage in wastewater due to higher ionic strength. Monovalent (Na+) and multivalent (Ca2+ and Mg2+) ion rejection was reported about 5 to 13%, and 23 to 40% respectively. Oil rejection varied from 96.2 to 99.2%.

14.
Drug Deliv Transl Res ; 8(3): 591-601, 2018 06.
Article in English | MEDLINE | ID: mdl-29423833

ABSTRACT

The oral bioavailability of felodipine (FEL) is very low, i.e., about 15%. This could be due to low water solubility and hepatic first-pass effect. The objective of the present study was to develop FEL microemulsion-based gel, to bypass the first pass effect, for buccal delivery. The optimized FEL microemulsion (OPT-MEF) was used to prepare buccoadhesive gels, with varying concentrations of hydroxypropyl methylcellulose (HPMC) E4M and polycarbophil (PCP), and evaluated. The cross-linking of the PCP gelling agent was done by adjusting the pH with a neutralizing agent, triethanolamine (TEA). The formulations, namely drug suspension, OPT-MEF, microemulsion-based buccal gel containing 1% w/v (MEF-E4M1), 2% w/v (MEF-E4M2), and 3% w/v (MEF-E4M3) of HPMC K4M and 1% w/v (MEF-PCP1), 2% w/v (MEF-PCP2), and 3% w/v (MEF-PCP3) of PCP were prepared and optimized on the basis of ex vivo permeation study, mucoadhesion force, and viscosity. The optimized buccal gel (MEF-PCP1) showed significantly higher (p < 0.01) permeation flux (J = 0.44 ± 0.16 mg/cm2/h), when compared with the drug suspension (J = 0.17 ± 0.14 mg/cm2/h). The permeation enhancement ratio of MEF-PCP1 was found to be 2.59 times higher than that of the aqueous suspension of the drug. The texture profile analysis of MEF-PCP1 was performed which showed spreadability (3.2 mJ), extrudability (151.8 mJ), hardness (13.8 g), and adhesiveness (41.0 g), and results indicated good spreadability and adhesiveness. The rheological study revealed the pseudoplastic flow behavior of MEF-PCP1 buccal gel. The Cmax value 9.21 ± 2.88 µg/ml of MEF-PCP1 gel was found to be significantly higher (P < 0.01) compared to the same dose administered by oral route (Cmax value 3.51 ± 1.74 µg/ml). The relative bioavailability (Fr) of the optimized MEF-PCP1 buccal gel was about 397.39% higher than that of oral route. In conclusion, consistent and effective buccal gel containing optimized FEL-loaded microemulsion, with improved buccal permeation and pharmacokinetic parameters was developed successfully to improve the bioavailability of FEL.


Subject(s)
Acrylic Resins/administration & dosage , Calcium Channel Blockers/administration & dosage , Felodipine/administration & dosage , Mouth Mucosa/metabolism , Acrylic Resins/chemistry , Acrylic Resins/pharmacokinetics , Adhesiveness , Administration, Buccal , Animals , Biological Availability , Calcium Channel Blockers/blood , Calcium Channel Blockers/chemistry , Calcium Channel Blockers/pharmacokinetics , Drug Stability , Emulsions , Felodipine/blood , Felodipine/chemistry , Felodipine/pharmacokinetics , Gels , Goats , Hydrogen-Ion Concentration , Permeability , Rats, Wistar , Viscosity
15.
Indian J Pharmacol ; 49(2): 145-154, 2017.
Article in English | MEDLINE | ID: mdl-28706327

ABSTRACT

Alzheimer's disease (AD) is a common, progressive, fatal neurodegenerative disorder, which will play an increasingly important role both socially and financially in the aging populations. Treatments for AD show modest improvements in cognition and global functioning among patients. Furthermore, the oral administration of treating AD has had some drawbacks that decrease the medication adherence and efficacy of the therapy. Transdermal drugs are proposed as an alternative remedy to overcome the disadvantages of current pharmaceutical dosage options for this chronic disorder. They could have different strengths, such as offering a stable diffusion of active substance, avoiding the first pass metabolism, and reducing system adverse reactions. This article reviews the technical principles, novel techniques of transdermal delivery drug, and prospects for future development for the management of cognitive and behavioral dysfunctions in AD patients.


Subject(s)
Alzheimer Disease/drug therapy , Neuroprotective Agents/administration & dosage , Administration, Cutaneous , Animals , Excitatory Amino Acid Antagonists/administration & dosage , Excitatory Amino Acid Antagonists/therapeutic use , Humans , Memantine/administration & dosage , Memantine/therapeutic use , Neuroprotective Agents/therapeutic use
16.
J Adv Res ; 8(6): 607-616, 2017 Nov.
Article in English | MEDLINE | ID: mdl-28794904

ABSTRACT

BCS class III drugs suffer from a drawback of low permeability even though they have high aqueous solubility. The objective of current work was to screen the suitability of glyceryl monooleate (GMO)/Pluronic F127 cubic phase liquid crystals precursors for permeation enhancement and in turn the bioavailability of tenofovir disoproxil fumarate (TDF), a BCS class III drug. Spray-drying method was used for preparation of TDF loaded liquid crystal precursors (LCP) consisting of GMO/Pluronic F127 and lactose monohydrate with an ability to in situ transform into stable cubic phases upon hydration. The quality by design (QbD) approach (Factorial design) was used for batch optimization. Spherical TDF loaded LCP as revealed by scanning electron microscopy photographs when hydrated and analyzed by small angle X-ray scattering confirmed formation of cubic phase. Differential scanning calorimetry and X-ray diffraction studies confirmed the molecular dispersion of TDF in polymer matrix and also suggested the conversion of TDF from crystalline to amorphous form. In vitro TDF release from prepared LCP showed controlled drug release over a period of 10 h. Further ex vivo studies revealed permeation enhancing activity of prepared LCP, which was highest when tested in presence of digestive enzyme extract. Thus, formulation of stable liquid crystal powder precursor can serve as an alternative for designing oral delivery system for drugs with low permeability.

17.
Drug Deliv ; 23(4): 1242-53, 2016 May.
Article in English | MEDLINE | ID: mdl-26697777

ABSTRACT

OBJECTIVE: To prepare and optimize the topical elastic liposome (EL)-loaded carbopol-980 gel of 5-Fluorouracil (5-FU) containing permeation enhancers (azone, propylene glycol (PG) and lauryl alcohol (LA)) and further evaluation for permeation flux of 5-FU, the activation energy and irritation in the rat skin. METHODS: EL formulations were prepared using phosphatidylcholine and varied surfactants (Span 60, Span 80 and Tween-80) by rotator evaporation method and optimized by experimental design. In vitro characterizations dictated the EL containing Span 80 (lipid:surfactant = 7:3) (EL3-S80) for further optimization of gel. Different gel formulations (5% w/w) with varying concentration (1-3%) of permeation enhancers were prepared and evaluated for viscosity, spreadability, the 5-FU permeation and deposition. The activation energy using the Franz diffusion cell and the plausible irritation using the Draize test were assessed on the albino rat and rabbit, respectively. RESULTS AND DISCUSSION: EL3-S80 was selected as an optimized EL owing to maximum desirability (0.99) and enhanced 5-FU flux (187.86 ± 14.1 µg/cm(2)/h). EL3-S80 suspension loaded gels (0.5%) revealed reduced viscosity leading to higher spreadability than blank gel. EL containing 3% azone in gel, EL containing 3% LA in gel and EL containing 3% PG in gel portrayed 187.86 ± 14.1, 117.7 ± 13.4 and 106.7 ± 7.3 µg/cm(2)/h as enhanced 5-FU flux values, respectively as compared to drug solution (8.8 ± 0.76 µg/cm(2)/h). Furthermore, reduced value of activation energy (2.63-folds) and the non-irritancy of gel could be effective and safe. CONCLUSION: ELA-3 gel formulation could be used as an effective and economic gel in cutaneous cancer and skin-related keratoses.


Subject(s)
Fluorouracil/administration & dosage , Gels/chemistry , Propylene Glycol/chemistry , Skin Neoplasms/drug therapy , Animals , Chemistry, Pharmaceutical , Drug Delivery Systems , Elasticity , Keratosis/metabolism , Liposomes , Rabbits , Rats , Viscosity
18.
J Food Sci ; 81(10): E2521-E2528, 2016 Oct.
Article in English | MEDLINE | ID: mdl-27649476

ABSTRACT

In this work, the crossflow microfiltration performance of rough beer samples was assessed using ceramic hollow-fiber (HF) membrane modules with a nominal pore size ranging from 0.2 to 1.4 µm. Under constant operating conditions (that is, transmembrane pressure difference, TMP = 2.35 bar; feed superficial velocity, vS = 2.5 m/s; temperature, T = 10 °C), quite small steady-state permeation fluxes (J* ) of 32 or 37 L/m2 /h were achieved using the 0.2- or 0.5-µm symmetric membrane modules. Both permeates exhibited turbidity <1 EBC unit, but a significant reduction in density, viscosity, color, extract, and foam half-life with respect to their corresponding retentates. The 0.8-µm asymmetric membrane module might be selected, its corresponding permeate having quite a good turbidity and medium reduction in the aforementioned beer quality parameters. Moreover, it exhibited J* values of the same order of magnitude of those claimed for the polyethersulfone HF membrane modules currently commercialized. The 1.4-µm asymmetric membrane module yielded quite a high steady-state permeation flux (196 ± 38 L/m2 /h), and a minimum decline in permeate quality parameters, except for the high levels of turbidity at room temperature and chill haze. In the circumstances, such a membrane module might be regarded as a real valid alternative to conventional powder filters on condition that the resulting permeate were submitted to a final finishing step using 0.45- or 0.65-µm microbially rated membrane cartridges prior to aseptic bottling. A novel combined beer clarification process was thus outlined.


Subject(s)
Beer , Ceramics , Food Analysis/methods , Filtration , Food Industry , Half-Life , Hydrogen-Ion Concentration , Hydrolysis , Membranes, Artificial , Porosity , Powders , Pressure , Temperature , Viscosity
19.
ACS Appl Mater Interfaces ; 7(41): 22918-26, 2015 Oct 21.
Article in English | MEDLINE | ID: mdl-26419767

ABSTRACT

A novel method based on beneficial phase reaction for developing composite membranes with high oxygen permeation flux and favorable stability was proposed in this work. Various Ce0.8Sm0.2O2-δ (SDC) + SrCO3+Co3O4 powders with different SDC contents were successfully fabricated into membranes through high temperature phase reaction. The X-ray diffraction (XRD) measurements suggest that the solid-state reaction between the SDC, SrCO3 and Co3O4 oxides occurred at the temperature for membrane sintering, leading to the formation of a highly conductive tetragonal perovskite phase SmxSr1-xCoO3-δ. The morphology and elemental distribution of the dual-phase membranes were characterized using back scattered scanning electron microscopy and energy dispersive X-ray spectroscopy (BSEM-EDX). The oxygen bulk diffusivity and surface exchange properties of the materials were investigated via the electrical conductivity relaxation technique, which supported the formation of conductive phases. The SDC+20 wt % SrCO3+10.89 wt % Co3O4 membrane exhibited the highest permeation flux among the others, reaching 0.93 mL cm(-2) min(-1) [STP = standard temperature and pressure] under an air/helium gradient at 900 °C for a membrane with a thickness of 0.5 mm. In addition, the oxygen permeation flux remained stable during the long-time test. The results demonstrate the beneficial phase reaction as a practical method for the development of high-performance dual-phase ceramic membranes.

20.
Daru ; 19(6): 433-9, 2011.
Article in English | MEDLINE | ID: mdl-23008689

ABSTRACT

BACKGROUND AND THE PURPOSE OF THE STUDY: Microemulsions are thermodynamically stable, clear dispersions of water, oil, surfactant, and cosurfactant. This study was aimed to develop flurbiprofen microemulsion for enhanced transdermal delivery and investigate the effects of different surfactants and cosurfactants on its delivery and phase behavior. METHOD: Various surfactant-cosurfactant mixtures in ratio of 2:1 (Smix) along with oleic acid (oil) were selected and phase diagrams were constructed. Six microemulsions each containing 5% drug, 5% oil, 56% Smix and 34% water, were prepared and compared for their permeation and phase behaviors to determine the effects of the type of Smix. RESULTS: In vitro transdermal permeation through rabbit skin of all microemulsions was high than saturated aqueous drug solution. Tween 20 and ethanol as Smix produced the highest flux amongst all the Smix, and were used to prepare formulations with different values of oil and Smix. While the type of surfactant did not affect the droplet size, propylene glycol as cosurfactant produced the largest droplets and highest viscosity. Decrease in oil or Smix concentration resulted in decrease of the droplet size and increase in permeation flux while decrease in viscosity also increased the permeation flux of microemulsions. Finally the selected microemulsion formulation comprising 5% flurbiprofen, 5% oleic acid, 46% Tween 20:ethanol (2:1) and 44% water, showed the highest transdermal flux and caused no skin irritation. CONCLUSION: Type of surfactant and cosurfactant affect both the phase behavior and transdermal drug delivery of microemulsion; and results of this study showed that they are promising vehicles for improved transdermal delivery and sustained action of flurbiprofen.

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