摘要 :
Iontophoresis is a physical drug delivery enhancing technique that was introduced at the beginning of the preceding century. For decades, iontophoresis research was focused on studying delivery-enhancing mechanisms and was limited...
展开
Iontophoresis is a physical drug delivery enhancing technique that was introduced at the beginning of the preceding century. For decades, iontophoresis research was focused on studying delivery-enhancing mechanisms and was limited to a few therapeutic applications (e.g. keratitis treatment, psoriasis treatment, tympanic membrane anesthesia for myringotomy). However, over the last few years, the spectrum of iontophoresis applicability has extended to include new target tissues and organs such as suprachoroidal space, nibbles and intestinal mucosa. Furthermore, the combination of iontophoresis with other approaches such as micmneedles, nanocarriers, and chemical enhancers has been widely explored to further optimize drug delivery. Moreover, the design of smart iontophoretic devices is rapidly evolving to allow the routine application of iontophoresis without medical assistance. This technological advancement is accompanied by remarkable progress in mathematical and computational simulations to predict iontophoretic drug delivery across different tissues. Therefore, this review addresses the latest advances in iontophoresis technology in terms of therapeutic applications, combinations with other drug delivery approaches, design of smart devices and mathematical modeling.
收起
摘要 :
For an effort to improve therapeutic property of metronidazole (MTZ) which is a drug of choice for protozoal infections such as luminal amoebiasis, sulfate conjugated metronidazole (MTZS) was prepared and evaluated as a colon-spec...
展开
For an effort to improve therapeutic property of metronidazole (MTZ) which is a drug of choice for protozoal infections such as luminal amoebiasis, sulfate conjugated metronidazole (MTZS) was prepared and evaluated as a colon-specific prodrug of MTZ. The apparent partition coefficient of MTZ was greatly reduced by the sulfate conjugation. While (bio)chemically stable in the contents of the upper intestine, MTZS was rapidly cleaved to liberate MTZ on incubation with the cecal contents of rats. MTZ liberated from MTZS metabolized quickly at least partly by a microbial nitroreductase, suggesting the relevance of the metabolism to bioactivation of MTZ for antimicrobial action. Consistent with the hypothesis, MTZS elicited antibacterial activity in the cecal contents, which was as potent as free MTZ. The systemic absorption of MTZS was very low after oral administration of MTZS. In parallel with this, whereas MTZ disappeared mostly during the transit of the proximal small intestine, a substantial amount of MTZS remained in the small intestine, moving down to the large intestine where it metabolized rapidly. In addition to the efficient colonic delivery of MTZS, MTZS markedly reduced the systemic absorption of MTZ. Taken together, MTZS may be a potential colon-specific prodrug of MTZ which possesses improved therapeutic and toxicological properties.
收起
摘要 :
Polymeric microneedle (MN) systems are interesting transdermal drug delivery systems because of their controlled drug delivery, tunable properties, and ease of patient self-administration. They are biocompatible and can easily and...
展开
Polymeric microneedle (MN) systems are interesting transdermal drug delivery systems because of their controlled drug delivery, tunable properties, and ease of patient self-administration. They are biocompatible and can easily and painlessly penetrate the stratum corneum, delivering their contents into the dermis where they can be adsorbed into systemic circulation. Polymeric MNs can facilitate appropriate therapeutic dosing by controlling the release kinetics of pre-loaded drugs, targeting specific tissues, or responding to changing physiological conditions. This can be accomplished by modifying the degradation and swelling profiles of the host polymer and the diffusion profiles of the encapsulated drugs. In this review various mechanisms of controlled drug delivery using polymeric MNs, including new strategies, applications, and their future outlook are summarized and evaluated.
收起
摘要 :
Background: Nanoemulsions are submicron-sized suspensions that are being studied extensively as pharmacological vehicles for enhancing the outcomes of drug delivery. Nanoemulsions are isotropic thermodynamic systems in which two i...
展开
Background: Nanoemulsions are submicron-sized suspensions that are being studied extensively as pharmacological vehicles for enhancing the outcomes of drug delivery. Nanoemulsions are isotropic thermodynamic systems in which two immiscible liquids (water and oil) are combined to form a single phase using pertinent surfactants. Nano-emulsions are resilient to sedimentation or creaming due to their nano-droplet size. Ostwald ripening represents the principal process accountable for the disintegration of nanoemulsion. Droplet diameters in nanoemulsions typically range from 20 to 500 nanometers. The diameter and surface parameters of nanoemulsion droplets play are of paramount significance in determining the bioactivity of the formulation. Nanoemulsion offers a promising future in various industries like cosmetology, diagnosis, pharmacological regimens, and biomedicine in the future. Methods: Pharmaceutical surfactants are utilized to synthesize nanoemulsions, which are Generally Regarded As Safe (GRAS). The stability of the NEs against coalescence mainly depends on the type and concentration of the surfactant employed. Nanoemulsions are formulated from a variety of oils, notably natural, semi-synthetic, and synthetic oils. Results: Over the past decade, various patents and clinical research have exemplified the applications of the NE system. Their application as a drug delivery entity in the ophthalmic, topical, transdermal, intranasal, intravenous, and oral routes is widely appreciated. Also, they have gained remarkable importance in the cosmetic industry. Conclusion: This review presents the importance of various components of NE and their importance in droplet formation and provides a brief insight into various drug administration routes of NE.
收起
摘要 :
Microneedles is the technique of drug delivery enhancement, which was primarily designed for facilitating percutaneous drug delivery. Started from the development of simple solid microneedles, providing microporation of stratum co...
展开
Microneedles is the technique of drug delivery enhancement, which was primarily designed for facilitating percutaneous drug delivery. Started from the development of simple solid microneedles, providing microporation of stratum corneum and therefore enhancement of topical drug delivery, for two decades the technique has progressed in various modifications such as hollow, coated, dissolving and hydrogel forming microneedles. In their turn, the modifications have resulted in new mechanisms of drug delivery enhancement and followed by the expansion of applicability range in terms of targeted tissues and organs. Thus, in addition to percutaneous drug delivery, microneedles have been considered as an efficient technique facilitating ocular, oral mucosal, gastrointestinal, ungual and vaginal drug administration. It is anticipated that the technique of microneedle-assisted drug delivery will soon become relevant for majority of organs and tissues.
收起
摘要 :
With the aim to reduce dosing frequency and to target drugs to cellular compartments actually in need of treatment, the design of drug delivery systems is becoming complementary to new drug discovery. The review highlights various...
展开
With the aim to reduce dosing frequency and to target drugs to cellular compartments actually in need of treatment, the design of drug delivery systems is becoming complementary to new drug discovery. The review highlights various drug/antigen delivery approaches comprising of vesicular and particulate nanocarriers that are associated with spectacular advantages like improved solubility and stability for poorly soluble drugs, good safety profile, versatility for encapsulating nearly all drugs, drug-release modulation, high drug payloads etc. In this review, light is shed on the remarkable potential of nanotechnology to provide more effective therapeutic and prophylactic approaches for the treatment and prevention for HIV/AIDS.
收起
摘要 :
Inflammatory bowel diseases, which largely comprise ulcerative colitis (UC) and Crohn's disease, are increasingly posing as a global threat because of the incompetence of the current therapy in the entire patient population. This ...
展开
Inflammatory bowel diseases, which largely comprise ulcerative colitis (UC) and Crohn's disease, are increasingly posing as a global threat because of the incompetence of the current therapy in the entire patient population. This necessitates the identification of alternative therapeutic molecules or their combinations, which may serve as effective first-line or maintenance therapeutics. In this quest, celecoxib, a selective cyclooxygenase-2 inhibiting nonsteroidal anti-inflammatory agent and curcumin, a natural antioxidant and anti-inflammatory agent, have both been found to be useful in alleviating UC. Furthermore, studies involving their combination have proved synergistic action of these two agents. In the current investigation, we have formulated pH-sensitive nanoparticles of curcumin–celecoxib combination as a potential therapy for UC. Synergistic action of the drug combination, delivery advantages of nanosized carriers, and pH-sensitive nature of the polymer were collectively hypothesized to reduce the overall toxicity and total dose of celecoxib and provide enhanced efficacy for mitigating UC. The hypothesis was confirmed in a UC model in rats, where pH-sensitive nanoparticles of the drug combination were found to be more efficacious than nanoparticles of either drugs or drug/s suspension. Further, the blank nanoparticles did not exhibit any therapeutic effect, thereby confirming efficacy of the drug combination for treating UC.
收起
摘要 :
Highlights ? Mucosal delivery systems differ in physicochemical and release characteristics. ? Versatile in vitro release methods are currently used for their characterisation. ? Compendial methods are used as a first approach whe...
展开
Highlights ? Mucosal delivery systems differ in physicochemical and release characteristics. ? Versatile in vitro release methods are currently used for their characterisation. ? Compendial methods are used as a first approach whenever applicable. ? Novel biorelevant methods are needed for the prediction of performance in vivo . Abstract In vitro dissolution/release tests are an important tool in the drug product development phase as well as in its quality control and the regulatory approval process. Mucosal drug delivery systems are aimed to provide both local and systemic drug action via mucosal surfaces of the body and exhibit significant differences in formulation design, as well as in their physicochemical and release characteristics. Therefore it is not possible to devise a single test system which would be suitable for release testing of such complex dosage forms. This article is aimed to provide a comprehensive review of both compendial and noncompendial methods used for in vitro dissolution/release testing of novel mucosal drug delivery systems aimed for ocular, nasal, oromucosal, vaginal and rectal administration.
收起
摘要 :
The recent work is based on the extraction and purification of natural gum from the bark of plant Terminalia elliptica (local name – Saaj) and the use of this gum to prepare pulsatile Drug Delivery System of Atenolol for the chro...
展开
The recent work is based on the extraction and purification of natural gum from the bark of plant Terminalia elliptica (local name – Saaj) and the use of this gum to prepare pulsatile Drug Delivery System of Atenolol for the chronotherapy of cardiovascular diseases. Three formulations CF1, CF2, CF3 of core tablets were prepared by direct compression technique by varying concentrations of crospovidone and evaluated. Formulation CF3 showed the highest 98.71% of drug release after 30 min was selected for press coating. Press coated tablets of Formulation F1 to F5 were prepared by direct compression technique using varying combinations of Saaj gum and Ethylcellulose in the ratio of 1:0, 3:1, 1:1, 1:3 and 0:1 respectively by taking CF3 as core in all. The extracted gum, powder blends, core tablets, and press coated tablets all were evaluated for their physicochemical properties. From the dissolution study of formulation F1 To F5 it was found that F2 having 3:1 combination of Saaj gum and EC shows a significant lag time of around 7 h by releasing only 4.09% of drug which followed by a bulk release of 97.61% of drug in between 7 to 8 h. The drug release kinetic studies of F2 shows the highest R 2 value i.e. 0.463 for the Korsmeyer Peppas model. The evaluation parameters like weight variation, hardness, friability, the thickness of F2 was found to be 555 ± 5, 6.6 ± 1.1 kg/cm 2 , 0.43 ± 0.1%, 5.7 ± 0.7 mm respectively, which meets with the official limits given in IP, BP, and USP.
收起
摘要 :
Khaled Greish speaks to Hannah Makin, Commissioning Editor: Khaled Greish is Associate Professor of Molecular Medicine, and head of the Nano-research unit, at Princes Al-Jawhara Center, Arabian Gulf University, Kingdom of Bahrain....
展开
Khaled Greish speaks to Hannah Makin, Commissioning Editor: Khaled Greish is Associate Professor of Molecular Medicine, and head of the Nano-research unit, at Princes Al-Jawhara Center, Arabian Gulf University, Kingdom of Bahrain. His previous appointments included Senior lecturer of Pharmacology at the University of Otago, New Zealand, and Assistant Professor of Pharmaceutical Chemistry at University of Utah (UT, USA). He has published >70 peer reviewed papers, and ten book chapters in the field of targeted anticancer drug delivery. Controlled Release Society (CRS) awarded him the CRS Postdoctoral Achievement Award in 2008 and in 2010; he was elected as member of the CRS College of Fellows. In recognition of his research, University of Otago awarded him “Early Career Awards for Distinction in Research” in 2014. His research focuses on nanomedicine, tumor vascular biology and anticancer drug discovery/development.
收起
原文获取