Levodopa Incorporation in Alginate Membranes for Drug Delivery Studies

2013 ◽  
Vol 749 ◽  
pp. 423-428
Author(s):  
Margarida Rosa Franco ◽  
Tânia Filipa Viana ◽  
Sara Biscaia ◽  
Paulo Bártolo

Parkinsons Disease (PD) is the second most common progressive neurodegenerative disorder and is referred as a leading cause of neurologic disability. The symptoms and signs of PD result from a decrease of dopamines level in the basal ganglia. Accordingly to this, exogenous substitution with dopamine agonists like levodopa, is used to correct the mechanical disorders at the early stages of the disease. Levodopa is referred as a standard in the treatment of PD. The modern studies of PD drug development and experimental therapeutics focuses on the concept of slowing and targeting the release of levodopa to prolong the therapeutic effect and reduce the number of administrations. The transdermal route was thought to be the best route for providing a progressive supply of levodopa to the systemic circulation. Alginate was chosen as a drug carrier because of its biocompatible and biodegradable properties and also because it has been widely used in drug delivery systems (DDS). The aim of this research work was to produce alginate membranes with and without levodopa. A solvent casting based methodology was used. Calcium chloride was assayed as crosslinking agent. Membranes were characterized using Differential Scanning Calorimetry (DSC) techniques. Drug release was evaluated using UV Spectrophotometry.

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1853-1863
Author(s):  
Shubhra Rai ◽  
Gopal Rai ◽  
Ashish Budhrani

Lipospheres represent a novel type of fat-based encapsulation system produced for the topical drug delivery of bioactive compounds. The goal of this research work was to develop lipospheres, including ketoprofen applied for topical skin drug delivery. Ketoprofen lipospheres were formulated by melt emulsification method using stearic acid and Phospholipon® 90G. The lipospheres were analysed in terms of particle size and morphology, entrapment efficiency, Differential scanning calorimetry, In-vitro drug release, In-vivo (Anti-inflammatory activity). Outcomes of research revealed that particle size was found to be 9.66 µm and entrapment efficiency 86.21 ± 5.79 %. In-vivo, the study of ketoprofen loaded lipospheres formulation shows a higher plain formulation concentration in plasma (5.61 mg/mL). For dermis, ketoprofen retention was 27.02 ± 5.4 mg/mL for the lipospheres formulation, in contrast to that of the plain formulation group (10.05 ± 2.8 mg/mL). The anti-inflammatory effect of liposphere drug delivery systems was assessed by the xylene induced ear oedema technique and compared with marketed products. Finally, it seems that the liposphere drug delivery system possesses superior anti-inflammatory activity as compared to the marketed product gel consistencies. Liposphere may be capable of entrapping the medicament at very high levels and controlling its release over an extended period. Liposphere furnishes a proper size for topical delivery as well as is based on non-irritating and non-toxic lipids; it’s a better option for application on damaged or inflamed skin.


2017 ◽  
Vol 25 (3) ◽  
pp. 241-246 ◽  
Author(s):  
Neha Mulchandani ◽  
Nimish Shah ◽  
Tejal Mehta

Chitosan is a natural polymer obtained from exoskeletons of crustaceans and polyvinyl alcohol (PVA) is a synthetic polymer which has excellent film forming ability along with non-toxic nature. The current work focuses on synthesizing a smart polymer by copolymerization of natural and synthetic polymers and exploring its applications in drug delivery. The copolymers were blended in different ratios and were synthesized using ammonium ceric nitrate as initiator and glutaraldehyde as a crosslinking agent which were converted to films by casting method. Amoxicillin, as a model drug was incorporated to the copolymerized films to study the in-vitro drug release. The films obtained were evaluated by varying the pH to study the pH responsive nature of films. Drug release studies were performed to obtain the release profile of drug; water uptake capacity of the copolymerized film were measured to determine the swelling behaviour of the films. The films were further characterized using Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and Differential Scanning Calorimetry (DSC) to identify the structural and morphological changes along with thermal transitions. The results indicate that the synthesized copolymers are pH responsive in nature having great potential for application in controlled and targeted drug delivery.


Materials ◽  
2019 ◽  
Vol 12 (11) ◽  
pp. 1830 ◽  
Author(s):  
Chaitra Venkatesh ◽  
Oran Clear ◽  
Ian Major ◽  
John G. Lyons ◽  
Declan M. Devine

Nanocomposite-based drug delivery systems with intrinsic controlled release properties are of great interest in biomedical applications. We report a novel polylactic acid (PLA)/halloysite nanotube (HNT) nanocomposite-based drug delivery system. PLA/HNT nanocomposites have shown immense potential for use in biomedical applications due to their favorable cyto- and hemo-compatibility. The objective of this study was to evaluate the release of active pharmaceutical ingredients (API) from PLA/HNT composites matrix and the effect of preloading the API into the lumen of the HNT on its release profile. Aspirin was used in this study as a model drug as it is a common nonsteroidal anti-inflammatory and antiplatelet agent widely used for various medical conditions. These two types of drug-loaded PLA/HNT nanocomposites were characterised by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), surface wettability and mechanical testing. Statistical analysis was conducted on numerical data. Drug entrapment and in vitro drug release studies were conducted using UV spectrophotometry. Results indicate that aspirin was successfully loaded into the lumen of HNT, which resulted in the sustained release of aspirin from the nanocomposites. Furthermore, the addition of HNT into the polymer matrix increased the mechanical properties, indicating its suitability as a drug-eluting reinforcing agent.


2007 ◽  
Vol 1008 ◽  
Author(s):  
Luciano Castaneda ◽  
Suzanne Pluskat ◽  
Darline Ky ◽  
Earry Te ◽  
Katarzyna Slowinska

AbstractIn a search for new drug delivery matrix, the synthesis of a novel collagen material based on tiopronin protected gold clusters (MPC) as a crosslinking agent is proposed. The structure of collagen matrix modified with MPC is studied using transmission electron microscope. The thermal properties are examined with differential scanning calorimetry. To assess the biocompatibility of the matrix, the cytotoxicity assays are conducted.


Author(s):  
Risvana Iqubal ◽  
Vimal Mathew ◽  
Kumar M. ◽  
Najiya Nasri K. V. ◽  
Safeetha Shamsudheen ◽  
...  

The poor penetration rate of the skin as a natural barrier makes transdermal drug delivery problematic. To increase transdermal dispersion of bioactives, electrophoresis, iontophoresis, chemical permeation enhancers, microneedles, sonophoresis, and vesicular systems such as liposomes, niosomes, elastic liposomes such as ethosomes, and transferosomes have all been used. Among these, transferosomes appear to be a promising option. Transferosomes are elastomeric or deformable vesicles that were originally discovered in the early 1990s. They're novel vesicular drug carrier system composed of phospholipid, surfactant, and water that improves transdermal drug delivery. Because of their low toxicity, biodegradability, ability to encapsulate both hydrophilic and lipophilic molecules, ability to prolong the drug's existence in the systemic circulation by encapsulation in vesicles, ability to target organs and tissues, and ability to reduce drug toxicity while increasing bioavailability, these vesicles are preferred over others. These vesicles undergo deformation, changes its shape and easily penetrates through the skin pores. There are two phases in any technique for preparing transferosomes. First, a thin film is hydrated before being sonicated to the required size; next, sonicated vesicles are homogenized by extrusion through a polycarbonate membrane. Transferosomes are evaluated for its entrapment efficiency, their drug content , in-vitro drug release, degree of deformability, turbidity, surface charge and morphology. Transferosomes are said to have a number of applications like delivery of vaccines,proteins, Anti-cancer drugs,anesthetics,herbal drugs and has better patient compliance,improved bio-availability and site-specific delivery and can serve as an emerging tool for transdermal delivery of almost all drugs and bio-actives.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 887
Author(s):  
Nutthapoom Pathomthongtaweechai ◽  
Chatchai Muanprasat

The small intestine provides the major site for the absorption of numerous orally administered drugs. However, before reaching to the systemic circulation to exert beneficial pharmacological activities, the oral drug delivery is hindered by poor absorption/metabolic instability of the drugs in gastrointestinal (GI) tract and the presence of the mucus layer overlying intestinal epithelium. Therefore, a polymeric drug delivery system has emerged as a robust approach to enhance oral drug bioavailability and intestinal drug absorption. Chitosan, a cationic polymer derived from chitin, and its derivatives have received remarkable attention to serve as a promising drug carrier, chiefly owing to their versatile, biocompatible, biodegradable, and non-toxic properties. Several types of chitosan-based drug delivery systems have been developed, including chemical modification, conjugates, capsules, and hybrids. They have been shown to be effective in improving intestinal assimilation of several types of drugs, e.g., antidiabetic, anticancer, antimicrobial, and anti-inflammatory drugs. In this review, the physiological challenges affecting intestinal drug absorption and the effects of chitosan on those parameters impacting on oral bioavailability are summarized. More appreciably, types of chitosan-based nanomaterials enhancing intestinal drug absorption and their mechanisms, as well as potential applications in diabetes, cancers, infections, and inflammation, are highlighted. The future perspective of chitosan applications is also discussed.


Author(s):  
Subhasri Mohapatra ◽  
Sourabh Jain ◽  
Karunakar Shukla

The object of present study was to formulate and evaluate MEM HCl loaded thermo sensitive in situ nanogel for 08 nasal delivery formulations. In present project a novel drug delivery system i.e. in situ polymeric gel was designed in the manner that the gel load MEM HCl in better concentration and it also incorporates penetration enhancer as a way to enhance the absorption of release drug from gel to the systemic circulation. In this research work Different Nanoparticles were (NP) prepared, using ionotropic gelation method with slight medication in which chitosan (0.4% w/v) was dissolved in aqueous acetic acid solutions (1 % v/v) (pH 6.1), while TPP (0.1% w/v) was dissolved in deionized water. Dried nanoparticles are incorporated with in situ gel. In situ gel was prepared by cold method using the solutions of Poloxamer-188 and Carbopol-934. From this study, it is concluded that, among all formulations prepared, NG8 was the best optimized formulation. Prepared gel can be used as promising nasal drug delivery system for the anti-Alzheimer drug MEM HCl, which enhance nasal residence time owing to increased viscosity and mucoadhesive characteristics; furthermore, it also exhibited a permeation enhancing effect.


Author(s):  
Mounika S Bharath ◽  
Bhushan R Rane ◽  
Ashish S Jain

A new drug delivery technology called transferosomes were came into existence which is an artificial vesicle designed to show the characteristics of a cell vesicle suitable for controlled and potentially directed drug delivery. Transferosome is a highly flexible and stress- responsive compound, complex compound and highly deformed vesicle with an aqueous core surrounded by the complex lipid bilayer thus enabling it to deliver both hydrophilic and hydrophobic drug. Urticaria is a general condition distinguished as brief erythematous and oedematous plaques or papules with defined erythematous borders and central clearing, identified as hives/wheals. Levocetirizine which is used for the treatment is a H1 anti histamine that is actively used in treatment of urticaria. The aim of the present research work was to investigate the potential of transferosome formulations for transdermal delivery of  levocetirizine. The transferosomes were formulated by lipid film hydration technique using Rotary vacuum Evaporator. In the present work levocetirizine vesicle was efficaciously formulated using an appropriate ratio of tween 80 and soya lecithin and was incorporated into gel since gel formulations are easy to administer and patient compliance. Levocetirizine transferosomes was evaluated for vesicle characteristicslike zeta potential, poly-dispersibility index, TEM, and stability study. Theaverage sizes of transferosome were found to be 566.6nm and poly dispersity index (PI) was found to be 0.532, zeta potential of the transferosome was found to be -2.3 mV which indicates that transferosome formulation is stable. Levocetirizine gel was prepared by using various concentrations of Carbopol 934 and is evaluated for their gel characteristics like pH, viscosity, Spreadability, extrudability, homogeneity, drug content, diffusion etc. Gel containing 2% Carbopol show best and promising results. Levocetirizine transferosomal gel were efficaciously formulated by utilizing levocetirizine transferosome which was prepared by thin film hydration method by using soya lecithin and tween 80 in the ratio 85:15. Other Oral formulation used in treatment for urticaria have disadvantage like poor bioavailability, 1st pass metabolism, patient non-compliance etc. Transferosome nano gel loaded with levocetirizine transferosome was found to be more effective than other oral formulations used in treatment for urticaria since transferosome are capable of passing through lipid layer and delivering drug into systemic circulation with maximum bioavailability.


Author(s):  
Preethi Sudheer ◽  
Koushik Y ◽  
Satish P ◽  
Uma Shankar M S ◽  
R S Thakur

As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new pharmacologically active lipophilic compounds that are poorly water soluble and solubility is one of the most important parameter to achieve desired concentration of drug in systemic circulation for therapeutic response. It is a great challenge for pharmaceutical scientist to convert those molecules into orally administered formulation with sufficient bioavailability.  Among the several approaches to improve oral bioavailability of these molecules, Self-micron emulsifying drug delivery system (SMEDDS) is one of the approaches usually used to improve the bioavailability of hydrophobic drugs. However, conventional SMEDDS are mostly prepared in a liquid form, which can have several disadvantages. Accordingly, solid SMEDDS (S-SMEDDS) prepared by solidification of liquid/semisolid self-micron emulsifying (SME) ingredients into powders have gained popularity. This article provides an overview of the recent advancements in S-SMEDDS such as methodology, techniques and future research directions.


2019 ◽  
Vol 26 (14) ◽  
pp. 2502-2513 ◽  
Author(s):  
Md. Iqbal Hassan Khan ◽  
Xingye An ◽  
Lei Dai ◽  
Hailong Li ◽  
Avik Khan ◽  
...  

The development of innovative drug delivery systems, versatile to different drug characteristics with better effectiveness and safety, has always been in high demand. Chitosan, an aminopolysaccharide, derived from natural chitin biomass, has received much attention as one of the emerging pharmaceutical excipients and drug delivery entities. Chitosan and its derivatives can be used for direct compression tablets, as disintegrant for controlled release or for improving dissolution. Chitosan has been reported for use in drug delivery system to produce drugs with enhanced muco-adhesiveness, permeation, absorption and bioavailability. Due to filmogenic and ionic properties of chitosan and its derivative(s), drug release mechanism using microsphere technology in hydrogel formulation is particularly relevant to pharmaceutical product development. This review highlights the suitability and future of chitosan in drug delivery with special attention to drug loading and release from chitosan based hydrogels. Extensive studies on the favorable non-toxicity, biocompatibility, biodegradability, solubility and molecular weight variation have made this polymer an attractive candidate for developing novel drug delivery systems including various advanced therapeutic applications such as gene delivery, DNA based drugs, organ specific drug carrier, cancer drug carrier, etc.


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