scholarly journals A Semi-Dissolving Microneedle Patch Incorporating TEMPO-Oxidized Bacterial Cellulose Nanofibers for Enhanced Transdermal Delivery

Polymers ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 1873 ◽  
Author(s):  
Ji Eun Song ◽  
Seung-Hyun Jun ◽  
Sun-Gyoo Park ◽  
Nae-Gyu Kang
Keyword(s):  
Bacterial Cellulose ◽  
Transdermal Delivery ◽  
Layer Structure ◽  
Drug Loading ◽  
Cellulose Nanofibers ◽  
Absorption Capacity ◽  
Water Soluble ◽  
Micro Channels ◽  
Backing Layer

Although dissolving microneedles have garnered considerable attention as transdermal delivery tools, insufficient drug loading remains a challenge owing to their small dimension. Herein, we report a one-step process of synthesizing semi-dissolving microneedle (SDMN) patches that enable effective transdermal drug delivery without loading drugs themselves by introducing TEMPO-oxidized bacterial cellulose nanofibers (TOBCNs), which are well dispersed, while retaining their unique properties in the aqueous phase. The SDMN patch fabricated by the micro-molding of a TOBCN/hydrophilic biopolymer mixture had a two-layer structure comprising a water-soluble needle layer and a TOBCN-containing insoluble backing layer. Moreover, the SDMN patch, which had a hole in the backing layer where TOBCNs are distributed uniformly, could offer novel advantages for the delivery of large quantities of active ingredients. In vitro permeation analysis confirmed that TOBCNs with high water absorption capacity could serve as drug reservoirs. Upon SDMN insertion and the application of drug aqueous solution through the drug inlet hole, the TOBCNs rapidly absorbed the solution and supplied it to the needle layer. Simultaneously, the needle layer dissolved in body fluids and the drug solution to form micro-channels, which enabled the delivery of larger quantities of drugs to the skin compared to that enabled by solution application alone.

scholarly journals Considerable Improvement of Ursolic Acid Water Solubility by Its Encapsulation in Dendrimer Nanoparticles: Design, Synthesis and Physicochemical Characterization

Nanomaterials ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 2196 ◽  
Author(s):  
Silvana Alfei ◽  
Anna Maria Schito ◽  
Guendalina Zuccari
Keyword(s):  
Ursolic Acid ◽  
Water Solubility ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Systemic Toxicity ◽  
Water Soluble ◽  
Design Synthesis ◽  
Pentacyclic Triterpenoid

Ursolic acid (UA) is a pentacyclic triterpenoid found in many medicinal plants and aromas endowed with numerous in vitro pharmacological activities, including antibacterial effects. Unfortunately, UA is poorly administered in vivo, due to its water insolubility, low bioavailability, and residual systemic toxicity, thus making urgent the development of water-soluble UA formulations. Dendrimers are nonpareil macromolecules possessing highly controlled size, shape, and architecture. In dendrimers with cationic surface, the contemporary presence of inner cavities and of hydrophilic peripheral functions, allows to encapsulate hydrophobic non-water-soluble drugs as UA, to enhance their water-solubility and stability, and to promote their protracted release, thus decreasing their systemic toxicity. In this paper, aiming at developing a new UA-based antibacterial agent administrable in vivo, we reported the physical entrapment of UA in a biodegradable not cytotoxic cationic dendrimer (G4K). UA-loaded dendrimer nanoparticles (UA-G4K) were obtained, which showed a drug loading (DL%) much higher than those previously reported, a protracted release profile governed by diffusion mechanisms, and no cytotoxicity. Also, UA-G4K was characterized by principal components analysis (PCA)-processed FTIR spectroscopy, by NMR and elemental analyses, and by dynamic light scattering experiments (DLS). The water solubility of UA-G4K was found to be 1868-fold times higher than that of pristine UA, thus making its clinical application feasible.

scholarly journals FORMULATION OF NANOPARTICLES OF TELMISARTAN INCORPORATED IN CARBOXYMETHYLCHITOSAN FOR THE BETTER DRUG DELIVERY AND ENHANCED BIOAVAILABILITY

2017 ◽  
Vol 10 (9) ◽  
pp. 236
Author(s):  
Upasana Yadav ◽  
Angshuman Ray Chowdhuri ◽  
Sumanta Kumar Sahu ◽  
Nuzhat Husain ◽  
Qamar Rehman
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Water Soluble ◽  
Bioavailability Enhancement ◽  
Water Soluble Drug ◽  
Efficient Option

  Objective: In this study, we have made an attempt to the developed formulation of nanoparticles (NPs) of telmisartan (TLM) incorporated in carboxymethyl chitosan (CMCS) for the better drug delivery and enhanced bioavailability.Materials and Methods: The NPs size and morphology were investigated by high-resolution transmission electron microscopy and field emission scanning electron microscopy, respectively. The crystal structures and surface functional groups were analyzed using X-ray diffraction pattern, and Fourier transform infrared spectroscopy, respectively.Results: To increase the solubility of TLM by targeted delivery of the drug through polymeric NPs is an alternative efficient, option for increasing the solubility. TLM nanosuspension powders were successfully formulated for dissolution and bioavailability enhancement of the drug. We focused on evaluating the influence of particle size and crystalline state on the in vitro and in vivo performance of TLM.Conclusion: In summary, we have developed a new approach toward the delivery of poorly water-soluble drug TLM by CMCS NPs. The particles having a good drug loading content and drug encapsulation efficiency. The cytotoxicity of the synthesized NPs is also very less.

Bacterial cellulose membranes as transdermal delivery systems for diclofenac: In vitro dissolution and permeation studies

2014 ◽  
Vol 106 ◽  
pp. 264-269 ◽  
Author(s):  
Nuno H.C.S. Silva ◽  
Artur Filipe Rodrigues ◽  
Isabel F. Almeida ◽  
Paulo C. Costa ◽  
Catarina Rosado ◽  
...  
Keyword(s):  
Bacterial Cellulose ◽  
Transdermal Delivery ◽  
Delivery Systems ◽  
In Vitro Dissolution ◽  
Permeation Studies ◽  
Cellulose Membranes

scholarly journals Study on the influence of technological factors on drug loading of poorly water-soluble drug on MCM-41 mesoporous carrier

Pharmacia ◽  
2020 ◽  
Vol 67 (4) ◽  
pp. 351-356
Author(s):  
Teodora Popova ◽  
Christina Voycheva ◽  
Borislav Tzankov
Keyword(s):  
Loading Rate ◽  
Drug Loading ◽  
In Vitro Release ◽  
Water Soluble ◽  
Technological Factors ◽  
Loading Process ◽  
Water Soluble Drug ◽  
Vitro Release ◽  
Mcm 41

The present study explored solvent impregnation drug loading process of the poorly soluble non-steroid anti-inflammatory drug indomethacin on MCM-41 type mesoporous silica carrier. Different technological factors that can influence drug-loading process as time of reaction, temperature, use of non-solvent as well as different ratios between drug and MCM-41 were studied. TEM and DLS were used to characterize physicochemical properties of obtained particles. The influence of drug-loading rate on dissolution process were studied using in-vitro release tests. Our results established that changes in explored technological factors could lead to different indomethacin loading. Moreover, the in-vitro release tests proved that drug loading rate had a direct influence on indomethacin release from MCM-41 particles. Our finding suggested that by tuning the main technological factors it would be possible different drug delivery systems with different drug loading rate to be obtained.

scholarly journals Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension

2019 ◽  
Vol 9 (3) ◽  
pp. 212-221 ◽  
Author(s):  
Aparna Bhalerao ◽  
Pankaj Prakash Chaudhari
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Cilinidipine is a fourth generation N and L-type calcium channel antagonists used alone or in combination with another drug to treat hypertension. Cilnidipine is poorly water -soluble, BCS class II drug with 6 to 30 percent oral bioavailability due to first pass metabolism. So to protect the drug from degradation and improve its dissolution, solid lipid nanoparticles were prepared. Glyceryl monostearate was selected as lipid while span 20: tween 20 were selected as surfactant blends. The formulations were evaluated for various parameters, as percent transmittance, drug content, percent encapsulation efficiency; percent drug loading, In vitro drug release and particle size. Optimized formulation was lyophilized using lactose as a cryo-protectant. The lyophilized formulation was evaluated for micromeritic properties, particle size and in vitro dissolution. It was further evaluated for DSC, XRD, and SEM. Percent encapsulation efficiency and percent drug loading of optimized formulation (F3) were 78.66percent and 9.44percent respectively. The particle size of F3 formulation without drug was 204 nm and with the drug was 214 nm. The particle size of the reconstituted SLN was 219 nm. In DSC study, no obvious peaks for cilnidipine were found in the SLN of cilnidipine indicated that the cilnidipine must be present in a molecularly dissolved state in SLN. In X-ray diffractometry absence of peaks representing crystals of cilnidipine in SLN indicated that the drug was in an amorphous or disordered crystalline phase in the lipid matrix. Thus, solid lipid nanoparticle formulation is a promising way to enhance the dissolution rate of cilnidipine. Keywords: Cilnidipine, Solid Lipid Nanoparticle, Hypertension

Preparation of Chitosan Nanoparticles for Protein Delivery by w/o/w Emulsion Solvent Evaporation and Simple Ionotropic Gelation Techniques

2007 ◽  
Vol 121-123 ◽  
pp. 751-754 ◽  
Author(s):  
Garnpimol C. Ritthidej ◽  
W. Pichayakorn ◽  
Chulalongkorn Kusonwiriyawong ◽  
V. Lipipun
Keyword(s):  
Protein Delivery ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Form Complex ◽  
Ionotropic Gelation

The purpose of this study was to prepare chitosan nanoparticles (CS NP) for controlled protein delivery. Two techniques, simple ionotropic gelation (method [I]) and w/o/w emulsion solvent evaporation containing ionotropic gelation (method [II]), were used to prepare CS NP. Tripolyphosphate (TPP) and Eudragit L100-55 (Eud) were used as anionic agents to form complex with cationic chitosan. Bovine serum albumin (BSA) was encapsulated into NP. The morphological characteristics, particle size and size distribution, protein entrapment efficiency, zeta potential, in vitro release, protein secondary structure and its integrity were investigated. The results showed that CS NP could be prepared by appropriate cationic and anionic ratios in both methods. Excess anionic agents resulted in particle aggregation of micron size. The median sizes of particles were between 0.127-0.273 mcm with method [I] provided the smallest size. The 0.02-0.10% BSA loaded preparations showed the same particle sizes and size distributions as blank preparations. SEM photomicrographs revealed that the obtained NP were spherical. Protein entrapment efficiency was between 47-84% and increased when decreasing the percentage of drug loading. The method [II] with TPP exhibited the highest protein entrapment efficiency, following by the method [II] with Eud and method [I] with TPP, respectively. The zeta potentials were positive. Prolonged in vitro protein release profiles were observed from all preparations of CS NP. After 10 days, the release was between 53-72%. Circular dichroism and SDS-polyaceylamide gel electrophoresis techniques confirmed that these processes did not have any destructive effect on the protein structure. Therefore these preparation techniques could be used to encapsulate water-soluble drugs, proteins, DNA, or antigens into CS NP as effective delivery carriers.

scholarly journals Alginate-amphotericin B nanocomplexes covered by nanocrystals from bacterial cellulose: physico-chemical characterization and in vitro toxicity

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Victória Soares Soeiro ◽  
Ricardo Silva-Carvalho ◽  
Daniela Martins ◽  
Pier Parpot ◽  
Denise Grotto ◽  
...  
Keyword(s):  
Bacterial Cellulose ◽  
Amphotericin B ◽  
Water Solubility ◽  
Chemical Characterization ◽  
Water Soluble ◽  
In Vitro Toxicity ◽  
Physico Chemical ◽  
Additional Protection ◽  
Anti Fungal

AbstractNanocomplexes systems made up natural poylymers have pharmacotechnical advantages such as increase of water solubility and a decrease of drugs toxicity. Amphotericin B (AmB) is a drug apply as anti-leishmanial and anti-fungal, however it has low water solubility and high toxicity, limiting its therapeutic application. With this in mind, the present study aimed to produce nanocomplexes composed by alginate (Alg), a natural polymer, with AmB covered by nanocrystals from bacterial cellulose (CNC). For this reason, the nanocomplexes were produced utilizing sodium alginate, amphotericin B in a borate buffer (pH 11.0). The CNC was obtained by enzymatic hydrolysis of the bacterial cellulose. To CNC cover the nanocomplexes 1 ml of the nanocomplexes was added into 1 ml of 0.01% CNC suspension. The results showed an ionic adsorption of the CNC into the Alg-AmB nanocomplexes surface. This phenomena was confirmed by an increase in the particle size and PDI decrease. Besides, nanocomplexes samples covered by CNC showed uniformity. The amorphous inclusion of AmB complex into the polysaccharide chain network in both formulations. AmB in the nanocomplexes was in supper-aggregated form and showed good biocompatibility, being significantly less cytotoxic in vitro against kidney cells and significantly less hemolytic compared to the free-drug. The in vitro toxicity results indicated the Alg-AmB nanocomplexes can be considered a non-toxic alternative to improve the AmB therapeutic effect. All process to obtain nanocomplexes and it coat was conduce without organic solvents, can be considered a green process, and allowed to obtain water soluble particles. Furthermore, CNC covering the nanocomplexes brought additional protection to the system can contribut advancement in the pharmaceutical.

Design and Characterization of Nanostructure Lipid Carrier for Transdermal Delivery of Pioglitazone

2018 ◽  
Vol 11 (4) ◽  
pp. 4185-4195
Author(s):  
Niket N Garude ◽  
Rachel B Geevarghese
Keyword(s):  
Drug Release ◽  
Transdermal Delivery ◽  
High Speed ◽  
Drug Loading ◽  
Skin Irritation ◽  
Systemic Availability ◽  
Transdermal Patch ◽  
Drug Release Profile ◽  
In Vitro Drug Release

Nanostructure Lipid Carrier (NLC) is one of the lipid-based drug delivery systems that are used as carrier for delivery of drugs. NLC are composed of mixture of solid lipid and liquid lipid, which form imperfect type of lipid matrix with improved drug loading capacity, drug release profile and stability. The aim of the present study was to develop and characterize nanostructure lipid carrier for transdermal delivery of pioglitazone (PZ) to overcome the problems related with oral route of administration and to improve systemic availability. NLC’s were prepared by high-speed homogenization method. Optimized NLC formulation was evaluated for particle size, percentage entrapment efficiency, surface morphology, DSC analysis, in-vitro drug release etc. The optimized NLC formulation was formulated as a transdermal patch and evaluated for in vitro drug release study and primary skin irritation study. In vivo hypoglycaemic activity of pioglitazone -NLC loaded transdermal patch was studied in comparison with its orally administered suspension. PZ- NLC loaded transdermal patch was found to be non-irritant and showed reduction in blood glucose level in a controlled manner up to 24 hrs.    

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