scholarly journals Recent Advances in Mupirocin Delivery Strategies for the Treatment of Bacterial Skin and Soft Tissue Infection

2021 ◽  
Vol 1 (1) ◽  
pp. 80-103
Author(s):  
Aishwarya Gangwar ◽  
Parveen Kumar ◽  
Ranjit Singh ◽  
Preeti Kush

Skin and soft tissue infections (SSTIs) have increased problematically in hospital and ambulatory settings due to the poor immunity of hosts and multidrug-resistant pathogens. Mupirocin (MUP), a global topical antibiotic, is used for the treatment of SSTIs caused by various pathogens due to its unique mechanism of action. However, the therapeutic efficiency of MUP is hampered due to the protein binding and drug resistance caused by frequent use. A combined report covering the various aspects of MUP, such as the synthesis of the novel formulation, loading of the drug, and application against various skin infections, is missing. This comprehensive review focuses on various novel drug delivery strategies such as composite biomaterials/scaffold, hydrogel dressings, liposomes, liposomal hydrogel, microparticles/microspheres, microsponges, nanocapsules, nanofibers, silicone-based adhesive patches, and topical sprays. The therapeutic effect of the MUP can be synergized by combining with other agents and using novel strategies. The objective is to enhance patient compliance, decrease the resistance, magnify the delivery of MUP, and overcome the limitations of conventional formulations. Moreover, the carriers/dressing materials are biocompatible, biodegradable, stimulate wound healing, protect the wound from external environmental contamination, adsorb the wound exudates, and are permeable to oxygen and moisture. This review will help researchers to explore further the treatment of various bacterial skin infections by using MUP-loaded novel formulations with better efficacy, utilizing the novel nanostructures or combinatorial methods.

2019 ◽  
Vol 7 (1) ◽  
pp. 24-38 ◽  
Author(s):  
Rupinder K. Dhamoon ◽  
Harvinder Popli ◽  
Madhu Gupta

Onychomycosis accounts for 50% of all nail disease cases and is commonly caused by dermatophytes. It was primarily considered a cosmetic problem but has been garnering attention lately due to its persistent nature and difficult treatment with relapses. With prolonged treatment duration and high cost involved in treating onychomycosis, several attempts have been made in overcoming the rigid nail barrier. The conventional treatment of onychomycosis involves oral and topical therapy. The oral antifungal agents though quite effective, are hepato-toxic and cause drug-drug interactions. Topical therapy is more patient compliant being devoid of such adverse effects but it suffers from another setback of improper nail penetration. Amorolfine and ciclopirox nail lacquers are popular market products. Since decades, efforts have been made to enhance topical delivery for efficiently treating onychomycosis. Mechanical, physical and chemical methods have been employed. Despite all the attempts made, the nail delivery issues are far from being solved. Recently, the focus has shifted to novel drug delivery systems like nanoparticles, microemulsions, polymeric films and nail lacquers for enhanced drug permeation and localized therapy. The research around the world is exploring their potential as effective treatment options. This review intends to further explore the novel delivery strategies to treat a persistent fungal infection like onychomycosis.


Author(s):  
Sagar T. Malsane ◽  
Smita S. Aher ◽  
R. B. Saudagar

Oral route is presently the gold standard in the pharmaceutical industry where it is regarded as the safest, most economical and most convenient method of drug delivery resulting in highest patient compliance. Over the past three decades, orally disintegrating tablets (FDTs) have gained considerable attention due to patient compliance. Usually, elderly people experience difficulty in swallowing the conventional dosage forms like tablets, capsules, solutions and suspensions because of tremors of extremities and dysphagia. In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. One such problem can be solved in the novel drug delivery system by formulating “Fast dissolving tablets” (FDTs) which disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of superdisintegrant or maximizing pore structure in the formulation. The review describes the various formulation aspects, superdisintegrants employed and technologies developed for FDTs, along with various excipients, evaluation tests, marketed formulation and drugs used in this research area.


Author(s):  
Jamal Basha D ◽  
Kumar P R ◽  
Ranganayakulu D

An oleo gum resin guggulu is a product which obtained as a result of gummosis from the bark of Commiphora wightii (Arnott) Bhandari [syn. Commiphoramukul (Hook. Ex Stocks) Family, Burseraceae]. It has been known for its immense applicability in the Ayurveda since time immemorial for the treatment of variety of disorders such as inflammation, gout, rheumatism, impotence, leprosy, obesity, and disorders of lipids metabolism. It is a mixture of phytoconstituents like terpenoids, steroids, flavonoids, guggultetrols, lignans, sugars, and amino acids. This review is an effort to compile all the information available on all of its chemical constituents which are responsible for its therapeutic potential, limitation of guggul extracts and the necessity of novel principles for gum guggul. Nowadays, Guggul is available as the marketed formulation for curing numerous clinical conditions and is accessible in combination with various other ingredients. Though conventional dosage form shows the dominance as patient compliance and easy availability, yet it has found to pose the problems like dose fluctuation, peak-valley effect, non-adjustment of the administered drug, invasiveness etc. Guggul lacks its desired effect due to its low bioavailability and water solubility. This makes it a partial or a deficient therapy for remedy of many signs and symptoms. Novel drug delivery system (NDDS), a new approach and has excluded many of drawbacks exhibited by conventional dosage forms. Some of the novel dosage forms of guggul has been formed like nanoparticles, nanovesicles, gugglusomes and proniosomal gel. But still, the novel formulations for guggul has its less outspread in the market. Guggul can be executed as a profitable drug using NDDS. There is a need to highlight the unidentified and unexplained facts about guggul so as to make it more efficacious and effective in terms of bioavailability and aqueous insolubility.


2020 ◽  
Vol 21 (11) ◽  
pp. 1085-1096 ◽  
Author(s):  
Rajesh Kumar Gupta ◽  
Girish R. Apte ◽  
Kiran Bharat Lokhande ◽  
Satyendra Mishra ◽  
Jayanta K. Pal

: With the emergence of the novel severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), the whole world is suffering from atypical pneumonia, which resulted in more than 559,047 deaths worldwide. In this time of crisis and urgency, the only hope comes from new candidate vaccines and potential antivirals. However, formulating new vaccines and synthesizing new antivirals are a laborious task. Therefore, considering the high infection rate and mortality due to COVID-19, utilization of previous information, and repurposing of existing drugs against valid viral targets have emerged as a novel drug discovery approach in this challenging time. The transmembrane spike (S) glycoprotein of coronaviruses (CoVs), which facilitates the virus’s entry into the host cells, exists in a homotrimeric form and is covered with N-linked glycans. S glycoprotein is known as the main target of antibodies having neutralizing potency and is also considered as an attractive target for therapeutic or vaccine development. Similarly, targeting of N-linked glycans of S glycoprotein envelope of CoV via carbohydrate-binding agents (CBAs) could serve as an attractive therapeutic approach for developing novel antivirals. CBAs from natural sources like lectins from plants, marine algae and prokaryotes and lectin mimics like Pradimicin-A (PRM-A) have shown antiviral activities against CoV and other enveloped viruses. However, the potential use of CBAs specifically lectins was limited due to unfavorable responses like immunogenicity, mitogenicity, hemagglutination, inflammatory activity, cellular toxicity, etc. Here, we reviewed the current scenario of CBAs as antivirals against CoVs, presented strategies to improve the efficacy of CBAs against CoVs; and studied the molecular interactions between CBAs (lectins and PRM-A) with Man9 by molecular docking for potential repurposing against CoVs in general, and SARSCoV- 2, in particular.


2021 ◽  
Vol 49 (1) ◽  
Author(s):  
Jane Namukobe ◽  
Peter Sekandi ◽  
Robert Byamukama ◽  
Moses Murungi ◽  
Jennifer Nambooze ◽  
...  

Abstract Background Rural populations in Uganda rely heavily on medicinal plants for the treatment of bacterial skin infections. However, the efficacy of these medicinal plants for their pharmacological action is not known. The study aimed at evaluating the antibacterial, antioxidant, and sun protection potential of Spermacoce princeae, Psorospermum febrifugum, Plectranthus caespitosus, and Erlangea tomentosa extracts. Methods The plant samples were extracted by maceration sequentially using hexane, dichloromethane, ethyl acetate, methanol, and distilled water. Antibacterial activity of each extract was carried out using an agar well diffusion assay against Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Klebsiella pneumonie, Streptococcus pyogenes, and Salmonella typhi. Acute dermal toxicity of the aqueous extract of S. princeae and P. febrifugum, and E. tomentosa was assessed in young adult healthy Wistar albino rats at a dose of 8000 and 10,000 mg/kg body weight. The antioxidant activity of each extract was carried out using a 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging assay. The sun protection factor was determined using Shimadzu UltraViolet-Visible double beam spectrophotometer between 290 and 320 nm. Results The plant extracts showed good antibacterial activity against the tested bacterial strains with minimum inhibitory concentration (MIC) ranging between 3.12 and 12.5 mg/ml. There was no significant change in the levels of creatinine, alanine aminotransferase, and aspartate aminotransferase in the rats even at a higher dose of 10,000 mg/kg, which was related to the results of biochemical analysis of the blood samples from the treated and control groups. The aqueous and methanol extracts of S. princeae showed potential antioxidant properties, with half maximal inhibitory concentration (IC50) values of 59.82 and 61.20 μg/ml respectively. The organic and aqueous extracts of P. caespitosus showed high levels of protection against Ultraviolet light with sun protection potential values ranging between 30.67 and 37.84. Conclusions The study demonstrated that the selected medicinal plants possessed good antibacterial, antioxidant, and sun protection properties. Therefore, the plants are alternative sources of antibacterial, antioxidant, and sun protection agents in managing bacterial skin infections.


2019 ◽  
Vol 87 (3) ◽  
pp. 20 ◽  
Author(s):  
Miléna Lengyel ◽  
Nikolett Kállai-Szabó ◽  
Vince Antal ◽  
András József Laki ◽  
István Antal

Microparticles, microspheres, and microcapsules are widely used constituents of multiparticulate drug delivery systems, offering both therapeutic and technological advantages. Microparticles are generally in the 1–1000 µm size range, serve as multiunit drug delivery systems with well-defined physiological and pharmacokinetic benefits in order to improve the effectiveness, tolerability, and patient compliance. This paper reviews their evolution, significance, and formulation factors (excipients and procedures), as well as their most important practical applications (inhaled insulin, liposomal preparations). The article presents the most important structures of microparticles (microspheres, microcapsules, coated pellets, etc.), interpreted with microscopic images too. The most significant production processes (spray drying, extrusion, coacervation, freeze-drying, microfluidics), the drug release mechanisms, and the commonly used excipients, the characterization, and the novel drug delivery systems (microbubbles, microsponges), as well as the preparations used in therapy are discussed in detail.


2012 ◽  
Vol 32 (6) ◽  
pp. 559-566 ◽  
Author(s):  
Yan Xu ◽  
Feng Zhi ◽  
Guangming Xu ◽  
Xiaolei Tang ◽  
Sheng Lu ◽  
...  

MDR (multidrug-resistance) represents a major obstacle to successful cancer chemotherapy and is usually accomplished by overexpression of P-gp (P-glycoprotein). Much effort has been devoted to developing P-gp inhibitors to modulate MDR. However, none of the inhibitors on the market have been successful. 1416 [1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (phenoprolamine hydrochloride)] is a new VER (verapamil) analogue with a higher IC50 for blocking calcium channel currents than VER. In the present paper, we examined the inhibition effect of 1416 on P-gp both in vitro and in vivo. 1416 significantly enhanced cytotoxicity of VBL (vinblastine) in P-gp-overexpressed human multidrug-resistant K562/ADM (adriamycin) and KBV cells, but had no such effect on the parent K562 and KB cells. The MDR-modulating function of 1416 was further confirmed by increasing intracellular Rh123 (rhodanmine123) content in MDR cells. Human K562/ADM xenograft-nude mice model verified that 1416 potentiates the antitumour activity of VBL in vivo. RT-PCR (reverse transcriptase-PCR) and FACS analysis demonstrated that the expression of MDR1/P-gp was not affected by 1416 treatment. All these observations suggest that 1416 could be a promising agent for overcoming MDR in cancer chemotherapy.


2008 ◽  
Vol 52 (4) ◽  
pp. 1522-1524 ◽  
Author(s):  
Eric Nuermberger ◽  
Sandeep Tyagi ◽  
Rokeya Tasneen ◽  
Kathy N. Williams ◽  
Deepak Almeida ◽  
...  

ABSTRACT PA-824 is a nitroimidazo-oxazine in clinical testing for the treatment of tuberculosis. We report that the novel combination of PA-824, moxifloxacin, and pyrazinamide cured mice more rapidly than the first-line regimen of rifampin, isoniazid, and pyrazinamide. If applicable to humans, regimens containing this combination may radically shorten the treatment of multidrug-resistant tuberculosis.


2014 ◽  
Vol 155 (35) ◽  
pp. 1383-1394 ◽  
Author(s):  
József Rácz ◽  
Róbert Csák

In this paper the authors summarize experience of a drug service provider with the injecting use of novel psychoactive substances. Among clients of the needle exchange programme of Blue Point Drug Counselling and Outpatient Centre, the authors observed the spread of the novel substances since 2009. The extensive spread of the novel substances caused substantial change in injecting use patterns, thus in the usage of the needle exchange programme. The novel psychoactive substances appeared consecutively, so that this setting gave a unique opportunity to observe and track the emergence of these substances. The authors summarize the characteristics which are important for medical practice (risks, frequent use, severe psychopathological conditions) as well as special risks associated with these substances (substances with unknown composition and effect). They highlight the importance and role of the early warning system, monitoring the online sources of information and testing of samples containing novel psychoactive substances. Orv. Hetil., 2014, 155(35), 1383–1394.


2020 ◽  
pp. 56-61
Author(s):  
Anh Mai Ba Hoang ◽  
Phuong Nguyen Thi Thanh ◽  
My Nguyen Thi Tra ◽  
Nguyen Le Thi Cao ◽  
Nam Tran Ngoc Khanh

Background: Bacterial skin infections are common due to the bacteral invasion into the skin and cause a variety of clinical manifestation. In order to assess the characteristics of this group, we conducted this study to evaluate the clinical and main subclinical features. Methods: A total of 95 patients were diagnosed with bacterial skin infections at Dermatology Clinic of Hue University of Medicine and Pharmacy Hospital from June 2015 to May 2016, of which 34 patients had some tests and 19 patients had samples for culture. Results: The age group of 16 - 30 years old was the most popular: 50.5%; High rate of patients came for consultation in winter (49.5%), most patients had no fever. For functional symptoms, pain accounted for the highest proportion: 71.6%. The most common skin lesion was nodule: 38.8%, the lower extremities were the most common position: 38.9%. Furuncle had the highest incidence: 45.3%. For main laboratory tests, most patients had a normal number of leucocyte: 71.4%; ESR increased by two times accounting for a rate of 20.6%; culture results showed Staphylococcus aureus being a highest percentage: 57.9%. Conclusion: Most skin infections localized and were less systemic effect, the most common agent was S. aureus. Keywords: infection, bacteria, skin, fever, S. aureus


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