Chitosan nanoparticles loading oxaliplatin as a mucoadhesive topical treatment of oral tumors: Iontophoresis further enhances drug delivery ex vivo

2020 ◽  
Vol 154 ◽  
pp. 1265-1275 ◽  
Author(s):  
Breno N. Matos ◽  
Maíra N. Pereira ◽  
Martha de O. Bravo ◽  
Marcilio Cunha-Filho ◽  
Felipe Saldanha-Araújo ◽  
...  
Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 527 ◽  
Author(s):  
Rancan ◽  
Contardi ◽  
Jurisch ◽  
Blume-Peytavi ◽  
Vogt ◽  
...  

Topical treatment of wound infections is often a challenge due to limited drug availability at the site of infection. Topical drug delivery is an attractive option for reducing systemic side effects, provided that a more selective and sustained local drug delivery is achieved. In this study, a poorly water-soluble antibiotic, ciprofloxacin, was loaded on polyvinylpyrrolidone (PVP)-based foils and nanofiber mats using acetic acid as a solubilizer. Drug delivery kinetics, local toxicity, and antimicrobial activity were tested on an ex vivo wound model based on full-thickness human skin. Wounds of 5 mm in diameter were created on 1.5 × 1.5 cm skin blocks and treated with the investigated materials. While nanofiber mats reached the highest amount of delivered drug after 6 h, foils rapidly achieved a maximum drug concentration and maintained it over 24 h. The treatment had no effect on the overall skin metabolic activity but influenced the wound healing process, as observed using histological analysis. Both delivery systems were efficient in preventing the growth of Pseudomonas aeruginosa biofilms in ex vivo human skin. Interestingly, foils loaded with 500 µg of ciprofloxacin accomplished the complete eradication of biofilm infections with 1 × 109 bacteria/wound. We conclude that antimicrobial-loaded resorbable PVP foils and nanofiber mats are promising delivery systems for the prevention or topical treatment of infected wounds.


2019 ◽  
Vol 56 (2) ◽  
pp. 396-398
Author(s):  
Georgeta Zegan ◽  
Daniela Anistoroaei ◽  
Elena Mihaela Carausu ◽  
Eduard Radu Cernei ◽  
loredana Golovcencu

Amoxicillin and clavulanic acid are two of the most commonly prescribed antibacterial worldwide for treating oral infectious diseases. Oral health is of big importance for well-being and general health. A few novel drug delivery systems were designed for oral treatment and prophylaxis of different diseases in the oral cavity. This work focused on the latest drug delivery development of the most common oral pathologies, namely, periodontitis, oral mucosal infections, dental caries and oral cancer. Herein we reveal the synthesis, characterization and application of chitosan nanoparticles for intracellular transport of the weakly cell-penetrating amoxicillin and clavulanic acid in order to improve their efficacy on bacterial infections.


2020 ◽  
Vol 10 (3) ◽  
pp. 185-196
Author(s):  
Sudha B. Patil ◽  
Syed Z. Inamdar ◽  
Kakarla R. Reddy ◽  
Anjanapura V. Raghu ◽  
Krishnamachari G. Akamanchi ◽  
...  

Background and Objectives: To develop electro-sensitive transdermal drug delivery systems (ETDDS) using polyacrylamide-grafted-pectin (PAAm-g-PCT) copolymer hydrogel for rivastigmine delivery. Methods: Free radical polymerization and alkaline hydrolysis technique was employed to synthesize PAAm-g-PCT copolymer hydrogel. The PAAm-g-PCT copolymeric hydrogel was used as a reservoir and cross-linked blend films of PCT and poly(vinyl alcohol) as rate-controlling membranes (RCMs) to prepare ETDDS. Results: The pH of the hydrogel reservoir was found to be in the range of 6.81 to 6.93 and drug content was 89.05 to 96.29%. The thickness of RCMs was in the range of 51 to 99 μ and RCMs showed permeability behavior against water vapors. There was a reduction in the water vapor transmission rate as the glutaraldehyde (GA) concentration was increased. The drug permeation rate from the ETDDS was enhanced under the influence of electric stimulus against the absence of an electric stimulus. The increase in flux by 1.5 fold was recorded with applied electric stimulus. The reduction in drug permeability observed when the concentration of GA was increased. Whereas, the permeability of the drug was augmented as an electric current was changed from 2 to 8 mA. The pulsatile drug release under “on– off” cycle of electric stimulus witnessed a faster drug release under ‘on’ condition and it was slow under ‘off’ condition. The alteration in skin composition after electrical stimulation was confirmed through histopathology studies. Conclusion: The PAAm-g-PCT copolymer hydrogel is a useful carrier for transdermal drug delivery activated by an electric signal to provide on-demand release of rivastigmine.


2020 ◽  
Vol 10 ◽  
Author(s):  
Sapna Saini ◽  
Sanju Nanda ◽  
Anju Dhiman

: Chitosan, a natural biodegradable polymer obtained from deacetylation of chitin, has been used as an approbative macromolecule for the development of various novel drug delivery systems. It is one of the most favorable biodegradable carriers for nanoparticulate drug delivery due to its intrinsic properties, such as biocompatibility, biodegradability, non-toxicity, availability of free reactive amino groups, and ease of chemical modification into different active derivatives. Furthermore, interesting physical properties (film-forming, gelling and thickening) make it a suitable candidate for formulations, such as films, microcapsules, beads, nanoparticles, nanofibres, nanogel and so on. Researchers have reported that chitosan nanoparticles act as a promising vehicle for herbal actives as they provide a superior alternative to traditional carriers and improve pharmaceutical efficiency. As no review of chitosan nanoparticles encapsulating herbal extracts and bioactives has been published till date, a maiden effort has been made to collate and review the use of chitosan nanoparticles for the entrapment of phytoconstituents to yield stable, efficient and safe drug delivery systems. Additionally, the paper presents a comprehensive account of the state-of the-art in fabricating herbal chitosan nanoparticles and their current pharmacological status. A list of patents on chitosan nanoparticles of herbal actives has also been included. This review is intended to serve as a didactic discourse for the formulation scientists endeavoring to develop advanced delivery systems for herbal actives.


2021 ◽  
Vol 8 (2) ◽  
Author(s):  
Yue Li ◽  
QingQing Leng ◽  
XianLun Pang ◽  
Huan Shi ◽  
YanLin Liu ◽  
...  

Abstract Dermal injury, including trauma, surgical incisions, and burns, remain the most prevalent socio-economical health care issue in the clinic. Nanomedicine represents a reliable administration strategy that can promote the healing of skin lesions, but the lack of effective drug delivery methods can limit its effectiveness. In this study, we developed a novel nano-drug delivery system to treat skin defects through spraying. We prepared curcumin-loaded chitosan nanoparticles modified with epidermal growth factor (EGF) to develop an aqueous EGF-modified spray (EGF@CCN) for the treatment of dermal wounds. In vitro assays showed that the EGF@CCN displayed low cytotoxicity, and that curcumin was continuously and slowly released from the EGF@CCN. In vivo efficacy on wound healing was then evaluated using full-thickness dermal defect models in Wistar rats, showing that the EGF@CCN had significant advantages in promoting wound healing. On day 12 post-operation, skin defects in the rats of the EGF@CCN group were almost completely restored. These effects were related to the activity of curcumin and EGF on skin healing, and the high compatibility of the nano formulation. We therefore conclude that the prepared nano-scaled EGF@CCN spray represents a promising strategy for the treatment of dermal wounds.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 544
Author(s):  
Miao Wang ◽  
Sung-Kyun You ◽  
Hong-Ki Lee ◽  
Min-Gu Han ◽  
Hyeon-Min Lee ◽  
...  

Docetaxel (DTX) has clinical efficacy in the treatment of breast cancer, but it is difficult to develop a product for oral administration, due to low solubility and permeability. This study focused on preparing a self-microemulsifying drug delivery system (SME) loaded with DTX-phospholipid complex (DTX@PLC), to improve the dissolution and gastrointestinal (GI) permeability of DTX. A dual technique combining the phospholipid complexation and SME formulation described as improving upon the disadvantages of DTX has been proposed. We hypothesized that the complexation of DTX with phospholipids can improve the lipophilicity of DTX, thereby increasing the affinity of the drug to the cell lipid membrane, and simultaneously improving permeability through the GI barrier. Meanwhile, DTX@PLC-loaded SME (DTX@PLC-SME) increases the dissolution and surface area of DTX by forming a microemulsion in the intestinal fluid, providing sufficient opportunity for the drug to contact the GI membrane. First, we prepared DTX@PLC-SME by combining dual technologies, which are advantages for oral absorption. Next, we optimized DTX@PLC-SME with nanosized droplets (117.1 nm), low precipitation (8.9%), and high solubility (33.0 mg/g), which formed a homogeneous microemulsion in the aqueous phase. Dissolution and cellular uptake studies demonstrated that DTX@PLC-SME showed 5.6-fold higher dissolution and 2.3-fold higher DTX uptake in Caco-2 cells than raw material. In addition, an ex vivo gut sac study confirmed that DTX@PLC-SME improved GI permeability of DTX by 2.6-fold compared to raw material. These results suggested that DTX@PLC-SME can significantly overcome the disadvantages of anticancer agents, such as low solubility and permeability.


Polymers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1285
Author(s):  
Louise Van Gheluwe ◽  
Igor Chourpa ◽  
Coline Gaigne ◽  
Emilie Munnier

Progress in recent years in the field of stimuli-responsive polymers, whose properties change depending on the intensity of a signal, permitted an increase in smart drug delivery systems (SDDS). SDDS have attracted the attention of the scientific community because they can help meet two current challenges of the pharmaceutical industry: targeted drug delivery and personalized medicine. Controlled release of the active ingredient can be achieved through various stimuli, among which are temperature, pH, redox potential or even enzymes. SDDS, hitherto explored mainly in oncology, are now developed in the fields of dermatology and cosmetics. They are mostly hydrogels or nanosystems, and the most-used stimuli are pH and temperature. This review offers an overview of polymer-based SDDS developed to trigger the release of active ingredients intended to treat skin conditions or pathologies. The methods used to attest to stimuli-responsiveness in vitro, ex vivo and in vivo are discussed.


Author(s):  
Abdul Baquee Ahmed ◽  
Iman Bhaduri

Objective: The objective of the present study was to chemical modification, characterization and evaluation of mucoadhesive potentiality of Assam bora rice starch as potential excipients in the sustained release drug delivery system. Methods: The starch was isolated from Assam bora rice and esterified using thioglycolic acid and characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and Nuclear magnetic resonance (NMR). The 10% w/v gel formulation based on modified bora rice starch loaded with irinotecan (0.6%) was prepared and evaluated for various rheological properties, ex-vivo mucoadhesion using goat intestine and in vitro drug release study in phosphate buffer pH 6.8.Results: The chemical modification was confirmed by FT-IR and NMR studies with the presence of the peak at 2626.74 cm-1 and a singlet at 2.51 respectively due to–SH group. Ex-vivo mucoadhesion studies showed 6.6 fold increases in mucoadhesion of the modified starch with compared to native starch (46.3±6.79g for native starch; 308.7±95.31g for modified starch). In vitro study showed 89.12±0.84 % of drug release after 6 h in phosphate buffer pH 6.8 and the release kinetics followed Non-Fickian diffusion.Conclusion: The modified Assam bora rice starch enhanced a mucoadhesive property of the native starch and thus, can be explored in future as a potential excipient for the sustained release mucoadhesive drug delivery system.


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