scholarly journals Mono- and Bi-Phasic Cellulose Acetate Micro-Vectors for Anti-Inflammatory Drug Delivery

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 87 ◽  
Author(s):  
Vincenzo Guarino ◽  
Rosaria Altobelli ◽  
Tania Caputo ◽  
Luigi Ambrosio ◽  
Sergio Caserta ◽  
...  

In recent years, different processing technologies have been engineered to fabricate capsules or particles with peculiar properties (e.g., swelling, pH-sensitive response) at the micro and sub-micrometric size scale, to be used as carriers for controlled drug and molecular release. Herein, the development of cellulose acetate (CA) micro-carriers with mono- (MC) or bi-phasic (BC) composition is proposed, fabricated via electrohydrodynamic atomization (EHDA)—an electro-dropping technology able to micro-size polymer solution by the application of high voltage electrostatic forces. Image analysis allows identification of the process parameters to optimize morphology, in terms of size distribution and shape. Meanwhile, an accurate rheological study has enabled investigating the interface between CA solutions with different viscosities to optimize BC systems. Release tests have confirmed that BC carriers can retain the drug more efficiently in acidic conditions, also providing a more gradual and sustained release until six days, with respect to MC carriers. Hence, all these results have proven that biphasic architecture significantly improves the capability of CA microcarriers to release ketoprofen lysinate, thus suggesting a new route to design core/shell systems for the retarded oral administration of anti-inflammatory drugs.

WARTA FARMASI ◽  
2017 ◽  
Vol 6 (1) ◽  
pp. 1-11
Author(s):  
Nur Saadah Daud ◽  
Musdalipah Musdalipah ◽  
Asriyanti Lamadari

ABSTRAK Aspirin termasuk dalam golongan Non Steroidal Anti Inflammatory Drugs (NSAIDs) yang banyak digunakan pada pengobatan nyeri ringan sampai sedang, antipiretik, anti inflamasi, serta anti koagulan. Pada penggunaan secara oral dapat menurunkan efektifitas obat akibat metabolisme lintas pertama. Alternatif untuk mengatasi masalah tersebut yaitu membuat sediaan topikal nanoemulsi aspirin. Nanoemulsi yaitu sistem emulsi yang transparan, tembus cahaya dan merupakan d ispersi minyak air yang distabilkan oleh lapisan film dari surfaktan dan ko-surfaktan, yang memiliki ukuran droplet 20 nm-500 nm. Penelitian ini bertujuan untuk membuat nanoemulsi aspirin dengan variasi konsentrasi etanol 96 % sebagai ko-surfaktan. Nanoemulsi aspirin dibuat dengan Virgin Coconut Oil (VCO) sebagai fase minyak, tween 80 sebagai surfaktan,dan etanol 96 % sebagai ko-surfaktan. Hasil penelitian mendapatkan 5 formula nanoemulsi jernih beraroma khas dengan nilai pH berkisar pada range 4,0-4,5 yang telah memenuhi pH normal kulit. dengan konsentrasi etanol 96 % yaitu 10 %, 15 %, 20 %, 25 % dan 30 %, dan dibuat 3 replikasi. Hasil uji stabilitas fisik menunjukkan bahwa kelima formula menghasilkan nanoemulsi yang stabil dan tidak terjadi pemisahan fase sesudah uji sentrifugasi dan cycling test dilakukan. Kata Kunci     : Nanoemulsi, Aspirin, Etanol 96%, Ko-surfaktan   ABSTRACT Acetosal known to be a part of the group medications called Non Steroidal Anti Inflammatory Drugs (NSAIDs) that was used for mild to moderate pain therapy, antipyretic, anti inflamation and anti coagulan. Oral administration of acetosal may decrease its effectiveness because of the first past metabolism problem. The purpose of this study was to formulate acetosal into nanoemulsion form for topical preparation as an alternative to avoid those problem with ethanol 96% as co-surfactant.  Nanoemulsion was an emultion system which transparent, glasslike, and comes from dispertion of water and oil stabilized by film-coated that made from surfactant and co-surfactant combination, which has droplet size around 20 nm-500 nm. Acetosal nanoemulsions were prepared with Virgin Coconut Oil (VCO) as oil phase, tween 80 as surfactant and ethanol 96 % as co-surfactant. There were 5 formulas of transparent acetosal nanoemultion. Their yield of pH were about 4,0-4,5 were met the normal skin’s pH. They were acetosal nanoemulsions with ethanol 96 % of 10%, 15%, 20%, 25%, and 30%. These five were stable and did not show the separation of phase after both centrifugation and cycling test. Keyword          : Nanoemulsion, Acetosal, Ethanol 96%, Co-Surfactan


2007 ◽  
Vol 73 (6) ◽  
pp. 618-624 ◽  
Author(s):  
William Newcomb ◽  
Amy Lincourt ◽  
William Hope ◽  
Thomas Schmelzer ◽  
Ronald Sing ◽  
...  

Compared with the open approach, laparoscopy has been shown to significantly reduce postoperative pain. Improving postoperative analgesia in laparoscopic surgery is an area of continued interest. The goal of this study was to compare the efficacy of local anesthetic infiltration with or without preoperative nonsteroidal anti-inflammatory drugs. Patients undergoing elective laparoscopic cholecystectomy were enrolled in an Institutional Review Board-approved, prospective, double-blinded, randomized, placebo-controlled comparison study. Patients were randomized into four groups: Group I, preoperative oral administration of a placebo medication and prein cision local infiltration of 40 mL of 0.5 per cent bupivicaine at trocar sites; Group II, preoperative oral administration of 50 mg of rofecoxib; Group III, preoperative oral administration of 50 mg of rofecoxib and preincision local infiltration of 40 mL of 0.5 per cent bupivicaine into skin, muscle, and peritoneum; and Group IV, preoperative oral administration of a placebo medication. Postoperative pain scores were assessed at 4 hours, 8 hours, 12 hours, and 24 hours using a visual analog scale. Postoperative analgesic use, complications, and length of stay were recorded. Statistical significance was defined as P < 0.05. Fifty-five patients (46 women and 9 men) were enrolled in this study and underwent a standardized, elective, laparoscopic cholecystectomy for mild, symptomatic cholelithiasis (96.4%) and gallbladder polyps (3.6%). No patient had pain immediately before surgery. Postoperative analgesic requests, visual analog scale results, incidence of postoperative vomiting at 4 hours, 8 hours, 12 hours, and 24 hours, in addition to length of stay, were not statistically different between the four groups. No complications occurred. The use of preoperative rofecoxib, 0.5 per cent bupivicaine infiltration, or both for postoperative analgesia did not decrease postoperative pain or decrease length of stay after laparoscopic cholecystectomy compared with placebo. Preoperative administration of an oral anti-inflammatory pain medication, infiltration of a local anesthetic, or both had no greater effect than placebo in controlling discomfort after a laparoscopic cholecystectomy. The challenge of preempting postoperative pain continues and will require further investigation.


2021 ◽  
Vol 142 ◽  
pp. 112014
Author(s):  
Kathryn E. Haley ◽  
Talal Almas ◽  
Saeed Shoar ◽  
Shan Shaikh ◽  
Maimoona Azhar ◽  
...  

2007 ◽  
Vol 105 (3) ◽  
pp. 251-257 ◽  
Author(s):  
Hai Yan Han ◽  
Takeshi Nabe ◽  
Nobuaki Mizutani ◽  
Masanori Fujii ◽  
Tetsuya Terada ◽  
...  

1978 ◽  
Vol 40 (01) ◽  
pp. 024-036 ◽  
Author(s):  
William Diamantis ◽  
William C Kohlhepp ◽  
Barbara Haertlein ◽  
John Melton ◽  
R Duane Sofia

SummaryMeseclazone and its major metabolite, 5-chlorosalicylic acid (5-CSA) have been shown to possess anti-inflammatory, analgesic and antipyretic activity. The comparative effects of these compounds on platelet aggregation were evaluated in vitro and ex vitro with acetylsalicylic acid (ASA). in vitro, meseclazone and ASA exhibited almost identical inhibitory potency of secondary phase ADP aggregation while 5-CSA was less effective. Moreover, collagen aggregation was inhibited by all three agents: ASA > meseclazone > 5- CSA. Thrombin-induced aggregation was inhibited to approximately the same extent by 5- CSA and ASA while meseclazone was inactive. The in vitro effects on the release-inducing aggregants were confirmed by ex vitro experiments in rats. These demonstrated that ASA and meseclazone inhibited collagen-induced aggregation 1 and 4 hr after oral administration although ASA was three to four times more active. ASA, but not meseclazone, was still effective 24 hr after administration. Bleeding times in rats 1 and 4 hr following oral administration of meseclazone and ASA were not altered. It is concluded that meseclazone and/or 5-CSA inhibit in vitro and ex vitro platelet aggregation initiated by the release reaction similar to ASA and other non-steroidal anti-inflammatory drugs.


2020 ◽  
Vol 11 (6) ◽  
pp. 363-372
Author(s):  
Jack Masterson ◽  
Brett Kluge ◽  
Aaron Burdette ◽  
George Lewis Sr

Background: Arthritis pain is primarily managed by nonsteroidal anti-inflammatory drugs (NSAIDs), such as diclofenac. Topical diclofenac gel is limited in efficacy due to its limited penetration through the skin. This study investigates the use of a multihour, wearable, localized, sonophoresis transdermal drug delivery device for the penetration enhancement of diclofenac through the skin. Materials & methods: A commercially available, sustained acoustic medicine (sam®) ultrasound device providing 4 h, 1.3 W, 132 mW/cm2, 3 MHz ultrasound treatment was evaluated for increasing the drug delivery of diclofenac gel through a human skin model and was compared with standard of care topical control diclofenac gel. Results: Sonophoresis of the diclofenac gel for 4 h increases diclofenac delivery by 3.8× (p < 0.01), and penetration by 32% (p < 0.01). Conclusion: Sustained acoustic medicine can be used as a transdermal drug-delivery device for nonsteroidal anti-inflammatory drugs.


2021 ◽  
pp. 51970
Author(s):  
Mariane A. Resende ◽  
Gabriele A. Pedroza ◽  
Lucia H. G. M. C. Macêdo ◽  
Ricardo Oliveira ◽  
Maria Amela‐Cortes ◽  
...  

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