scholarly journals Design and evaluation of a bioadhesive film for transdermal delivery of propranolol hydrochloride

2011 ◽  
Vol 61 (3) ◽  
pp. 271-282 ◽  
Author(s):  
Bazigha Rasool ◽  
Uday Aziz ◽  
Omar Sarheed ◽  
Alaa Rasool
Keyword(s):  
Delivery System ◽  
Transdermal Delivery ◽  
Skin Irritation ◽  
Chitosan Film ◽  
Penetration Enhancers ◽  
Propranolol Hydrochloride ◽  
Moisture Uptake ◽  
Rat Skin ◽  
Uptake Capacity ◽  
Dermal Delivery

Design and evaluation of a bioadhesive film for transdermal delivery of propranolol hydrochlorideThe objective of the study was to develop a suitable trans-dermal delivery system for propranolol hydrochloride (PPL)viaemploying chitosan as a film former. Drug concentration uniformity, thickness, moisture uptake capacity and skin bioadhesion of the films were characterized. The effects of chitosan and PPL concentration and different penetration enhancers on the release and permeation profiles from the films were investigated. Skin irritation of the candidate film was evaluated. Chitosan film (PPL 2 mg cm-2, chitosan 2 %,m/m, cineol 10 %,m/m) was found nonirritant and achieved 88.2 % release after 8 hours in phosphate buffer. Significant high (p< 0.001) permeation of PPL through rat skin was obtained using this film compared to the film without enhancer (about 8 times enhancement factor), making it a promising trans-dermal delivery system for PPL.

scholarly journals Design and Evaluation of Chitosan films for Transdermal delivery of Glimepiride

2018 ◽  
pp. 13-25
Author(s):  
Syed Ata Ur Rahman ◽  
Neeraj Sharma
Keyword(s):  
Delivery System ◽  
Transdermal Delivery ◽  
Inclusion Complexation ◽  
Penetration Enhancers ◽  
In Vivo Studies ◽  
Skin Barrier Function ◽  
Antidiabetic Therapy ◽  
Transdermal Delivery System ◽  
Chitosan Films

Glimepiride is a third generation oral antidiabetic sulphonylurea drug frequently prescribed to patients of type 2 diabetes. However, its oral therapy is encountered with bioavailability problems due to its poor solubility leading to irreproducible clinical response, in addition to adverse effects like dizziness and gastric disturbances. As a potential for convenient, safe and effective antidiabetic therapy, the rationale of this study was to develop a transdermal delivery system for glimepiride. Chitosan polymer was utilized in developing transdermal films for glimepiride. Chitosan has film forming ability, bioadhesive and absorption enhancing properties. Aiming at optimizing the drug delivery and circumventing the skin barrier function, inclusion complexation of glimepiride with beta-cyclodextrin (β-CyD) as well as the use of several conventional penetration enhancers were monitored for augmenting the drug flux. The physical and mechanical properties of the prepared films were investigated using tensile testing, IR spectroscopy and X-ray diffractometry. Release studies revealed adequate release rates from chitosan films. Permeation studies through full thickness rat abdominal skin were conducted. High flux values were obtained from films comprising a combination of the drug with limonene and ethanol as well as from films containing glimepiride-β-CyD complex. In vivo studies on diabetic rats for selected formulae revealed a marked therapeutic efficacy sustained for about 48 hours. The above-mentioned results shed light on feasibility of utilizing chitosan as an effective, safe transdermal delivery system for glimepiride characterized by increased patient compliance and better control of the disease.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF TRANSDERMAL DELIVERY SYSTEM OF DOXAZOSIN MESYLATE

2019 ◽  
Vol 11 (1) ◽  
pp. 43 ◽  
Author(s):  
Madhur Kulkarni ◽  
Vishakha Hastak ◽  
Supriya Jadhav
Keyword(s):  
Delivery System ◽  
Transdermal Delivery ◽  
Skin Irritation ◽  
Stability Studies ◽  
Accelerated Stability ◽  
In Vitro Permeation ◽  
Folding Endurance ◽  
Transdermal Delivery System

Objective: The study involved development of transdermal delivery system (TDDS) of doxazosinmesylate (doxa) to achieve effective systemic delivery of the drug.Methods: TDDS of doxa was prepared using hydroxypropyl methyl cellulose (HPMC) K100LV and polyvinyl pyrrolidone (PVP) K30 in 3:1 ratio solvent casting method. The formulation was evaluated for folding endurance, moisture uptake, pH, drug content and in vitro permeation. Various permeation enhancers were incorporated at 5% w/w concentration into the patch formulationto study their impact on the drug permeation. The TDDS made with Transcutol® as an enhancer was subjected to accelerated stability studies and in vivo skin irritation studies.Results: The developed TDDS showed folding endurance of 170, moisture uptakeof 15.7%, pH of 6.3, and drug content of 99±1.1% and 66% in vitro permeation of doxa over 24h. The effect of various enhancers expressed in terms of average flux can be summarized as Transcutol® (10.6±2.1 µg/cm2h)>dimethyl sulfoxide(10.17±1.2 µg/cm2h)>benzyl alcohol (9.55±1.3 µg/cm2h)>no enhancer (8.86±1.1 µg/cm2h)>dimethyl isosorbide (8.21±1.5 µg/cm2h)>Isostearic acid (7.82±1.4 µg/cm2h)>propylene carbonate (7.67±1.4 µg/cm2h)>oleic acid (7.12 µg±0.8/cm2h). The formulation was found to be stable during the accelerated stability studies. In vivo studies indicated absence of skin irritation effect the TDDS containing Transcutol®.Conclusion: TDDS of doxa comprising HPMC K100LV and PVPK30 in the ratio of 3:1 and 5% Transcutol® could serve as a potential TDDS in the treatment of benign prostatic hyperplasia (BPH) and hypertension.

scholarly journals Self-Dissolving Microneedle Arrays for Transdermal Absorption Enhancement of Human Parathyroid Hormone (1-34)

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 215 ◽  
Author(s):  
Chihiro Naito ◽  
Hidemasa Katsumi ◽  
Tomoko Suzuki ◽  
Ying-shu Quan ◽  
Fumio Kamiyama ◽  
...  
Keyword(s):  
Parathyroid Hormone ◽  
Transdermal Delivery ◽  
Subcutaneous Injection ◽  
Skin Irritation ◽  
Absorption Enhancement ◽  
Human Parathyroid Hormone ◽  
Rat Skin ◽  
Treatment Of Osteoporosis ◽  
Molding Method ◽  
Microneedle Arrays

Human parathyroid hormone (1-34) (PTH) has been widely used as the subcutaneous injection formulation for the treatment of osteoporosis. In the present study, we developed an efficient transdermal delivery system of PTH by using dissolving microneedle arrays (MNs) composed of hyaluronic acid (HA) for the treatment of osteoporosis. PTH-loaded MNs, with needle length 800 µm, were fabricated via a micro-molding method. The stability of PTH in MNs was found to be 6-fold higher than that of PTH solution when stored at room temperature (15–20 °C) for one month. Micron-scale pores were clearly visible in rat skin following application of PTH-loaded MNs. PTH-loaded MNs were completely dissolved by 60 min following application to rat skin. The bioavailability (BA) of PTH relative to subcutaneous injection was 100 ± 4% following application of PTH-loaded MNs in rats. In addition, PTH-loaded MNs were found to effectively suppress decreases in bone density in a rat model of osteoporosis. Furthermore, no skin irritation was observed at the site of application in rats. These findings indicate that our dissolving MNs have a potential use in formulations for the transdermal delivery of PTH and for the treatment of osteoporosis.

Effect of Penetration Enhancers on the Transdermal Delivery of Bupranolol Through Rat Skin

Drug Delivery ◽  
2005 ◽  
Vol 12 (3) ◽  
pp. 165-169 ◽  
Author(s):  
R. Jayachandra Babu ◽  
Jayanta Kumar Pandit
Keyword(s):  
Transdermal Delivery ◽  
Penetration Enhancers ◽  
Rat Skin

Identifying underlying issues related to the inactive excipients of transfersomes based drug delivery system

2020 ◽  
Vol 26 ◽  
Author(s):  
Drashti Patel ◽  
Bappaditya Chatterjee
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Delivery ◽  
Systemic Availability ◽  
Drug Penetration ◽  
Skin Damage ◽  
Variable Effect ◽  
Practical Factors ◽  
Edge Activator

: Transfersomes are bilayer vesicles composed of phospholipid and edge-activators, which are mostly surfactant. Transfersomes based drug delivery system has gained a lot of interest of the pharmaceutical researchers for their ability to improve drug penetration and permeation through the skin. Transdermal drug delivery via transfersomes has the potential to overcome the challenge of low systemic availability. However, this complex vesicular system has different issues to consider for developing a successful transdermal delivery system. One of the major ingredients, phospholipid has versatile sources and variable effect on the vesicle size and drug entrapment in transfersomes. The other one termed as edge-activator or surfactant has some crucial consideration of skin damage and toxicity depending upon its type and concentration. A complex interaction between type and concentration of phospholipid and surfactant was observed, which affect the physicochemical properties of transfersomes. This review focuses on the practical factors related to these two major ingredients such as phospholipid and surfactant. The origin, purity, desired concentration, the susceptibility of degradation, etc. are the important factors for selecting phospholipid. Regarding surfactants, the major aspects are type and desired concentration. A successful development of transfersomes based drug delivery system depends on the proper considerations of these factors and practical aspects.

Gel-based Microemulsion Design and Evaluation for Topical Application of Rivastigmine

2020 ◽  
Vol 21 (4) ◽  
pp. 298-304
Author(s):  
Chih-Wen Fang ◽  
Ling-Chun Tsai ◽  
Yaw-Syan Fu ◽  
Ting-Yu Cheng ◽  
Pao-Chu Wu
Keyword(s):  
Topical Application ◽  
Skin Irritation ◽  
Topical Administration ◽  
Lag Time ◽  
Enhancement Effect ◽  
Microemulsion Formulation ◽  
Rat Skin ◽  
Glycol Monobutyl Ether ◽  
Loading Amount ◽  
Hydrophilic Gel

Objective: The aim of the present study was to design nanocarriers for the topical application of rivastigmine. Methods: The effect of cosurfactants, hydrophilic gel and loading amount on the permeability of rivastigmine through rat skin was evaluated. Skin irritation tests and stability tests were performed to evaluate the utility of tested formulations. Results: The results showed that the microemulsion formation and characteristics of drug-loaded formulations were related to many parameters of the components. When using microemulsion systems as a vehicle, the permeation rate remarkably increased about 13.2~24.3-fold and the lag time was significantly shortened from 24 h to 4.7 h. Formulations containing a cosurfactant of Diethylene Glycol Monobutyl Ether (DEGBE) showed higher enhancement effect, while increasing the loading dose from 0.5% to 5% further increased the flux about 2.1-fold and shortened the lag time. Conclusion: The drug-loaded experimental formulation did not cause skin irritation and had good stability at 20ºC and 40ºC storage for at least 3 months. The result showed that gel-based microemulsion formulation could be a promising approach for topical administration.

scholarly journals Size-Tunable Paclitaxel Nanoparticles Stabilized by Anionic Phospholipids for Transdermal Delivery Applications

2020 ◽  
Vol 15 (3) ◽  
pp. 1934578X1990068
Author(s):  
Noriyuki Uchida ◽  
Masayoshi Yanagi ◽  
Hiroki Hamada
Keyword(s):  
Stratum Corneum ◽  
Transdermal Delivery ◽  
Skin Tissue ◽  
Composite Nanoparticles ◽  
Rat Skin ◽  
Cooling Process ◽  
Anionic Phospholipid ◽  
Anionic Phospholipids ◽  
Subsequent Heating

Composite nanoparticles composed of an anionic phospholipid of 1,2-dipalmitoyl-sn-glycero-3-phosphorylglycerol (DPPG) and paclitaxel (PTX) were successfully prepared by mixing them in water followed by a subsequent heating/cooling process. The size of DPPG-PTX nanoparticle could be easily tuned by ultrasonic fragmentation. Upon addition of small-sized fluorescently labeled paclitaxel (FLPTX) nanoparticles with DPPG (DPPG-FLPTX) to rat skin tissue, part of the FLPTX molecules permeated to the stratum corneum.

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