Aseklofenak içeren kendiliğinden nanoemülsiyon oluşturan sistemlerin geliştirilmesi ve antienflamatuvar etkinliğin sıçanlarda değerlendirilmesi
Abstract
Amaç: Aseklofenak yüklü kendiliğinden nanoemülsifiye olan sistemlerin karragenle tetiklenen sıçan pençe ödemi yöntemi ile antiinflamatuar aktivitesinin belirlenmesi ve midede peteşi kontrolü ile sistemlerin gastrik ülserojenik aktivite olup olmadığının araştırılması amaçlanmıştır.
Araçlar ve Yöntem: Çalışma randomize kontrollü ve prospektif olarak planlandı. Çalışmada 200-300 g arasındaki ağırlıklarda, Wistar, albino erkek sıçanlar kullanılmıştır. Oral gavajla verilen aseklofenak dozu 10 mg/kg’dır. Çalışma grupları 17 gruba ayrılmıştır (n=6) ve her birine oral gavaj uygulanmıştır (100 g sıçan için 0,5 mL örnek). Uygulama sonrası pençe hacimleri pletismometre ile 0., 90., 180., 270. ve 360. dakikalarda ölçülmüştür. Akut toksik etki incelenmiş ve 48 saat sonra mortalite varlığı kaydedilmiştir. Aseklofenağın gastrik ülserojenik etkisini incelemek için, sıçanların mideleri çıkarılmış ve peteşi varlığı incelenmiştir.
Bulgular: Bütün Aseklofenak grupları 180. dakikada maksimum ödem inhibisyonu göstermiştir. Geliştirilen sistemin inhibisyonu (ND-1+AC kodlu) tüm ölçülen zaman noktalarında diğer gruplarla kıyaslandığında daha yüksektir (p<0,001) ve ülserojenik etki görülmemiştir. Sistemlerin hiçbiri peteşiye neden olmamıştır. Hiçbir grup akut toksik etki göstermemiştir.
Sonuç: Yapılan bu çalışma ile geliştirilen aseklofenak içeren sistemin etkili olduğu ve medikal tedavide alternatif bir ilaç veriliş sistemi olduğu gösterilmiştir.
Keywords
Supporting Institution
Gazi Üniversitesi Bilimsel Araştırma Projeleri Birimi
Project Number
02/2010-47
References
- 1. Elnaggar YSR, El-Massik MA, Abdallah OY. Self-nanoemulsifying drug delivery systems of tamoxifen citrate: Design and optimization. Int J Pharm. 2009; 380: 133-41.
- 2. Ren F, Jing Q, Cui J, Chen J, Shen Y. Self-nanoemulsifying drug delivery system (SNEDDS) of anethole trithione by combined use of surfactants. J Dispersion Sci Technol. 2009; 30: 664-70.
- 3. Xi J, Chang Q, Chan CK, et al. Formulation development and bioavailability evaluation of a self-nanoemulsified drug delivery system of oleanolic acid. AAPS Pharm Sci Tech. 2009; 10(1): 172-82.
- 4. Shaji J, Lodha S. Response surface methodology for the optimization of celecoxib self-microemulsifying drug delivery system. Indian J Pharm Sci. 2008; 70: 585-90.
- 5. Tang J, Sun J, Cui F, Zhang T, Liu X, He Z. Self-emulsifying drug delivery systems for improving oral absorption of Ginkgo Biloba extracts. Drug Delivery. 2008; 15: 477-84.
- 6. Özbek H, Öztürk A. Antienflamatuvar Etkinliğin Ölçülmesinde Kullanılan Yöntemler. Van Tıp Dergisi. 2003; 10 (1):23-8.
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- 8. Süleyman H, Demirezer LÖ, Kuruüzüm A, et al. Antiinflammatory effect of the aqueous extract from Rumex patientia L. roots. J. Ethnopharmacol. 1999; 65: 141-8.
- 9. Rimbau V, Cerdan C, Vila R, et al. Antiinflammatory activity of some extracts from plants used in the traditional medicine of North-African countries (II). Phytother Res. 1999; 13: 128-32.
- 10. Vijayakumar CS, Viswanathan S, Reddy MK, et al: Anti-inflammatory activity of usnic acid. Fitoterapia. 2000; 71: 564-6.
- 11. Akkuş Arslan Ş. Kendiliğinden nanoemülsifiye olan ilaç taşıyıcı sistemler. Gazi Üniversitesi / Sağlık Bilimleri Enstitüsü / Farmasötik Teknoloji Ana Bilim Dalı, Doktora tezi, Ankara, Türkiye, 2013.
- 12. Nagda C, Chotai NP, Patel U, et al. Preparation and characterization of spray-dried mucoadhesive microspheres of aceclofenac. Drug Dev Ind Pharm. 2009; 35(10): 1155-66.
- 13. Shaikh IM, Jadhav SI, Jadhav KR, Kadam VJ, Pisal SS. Aceclofenac organogels: In vitro and in vivo characterization. Curr Drug Delivery. 2009; 6: 1-7.
- 14. Yesilada E, Gurbuz I. Evaluation of the antiulcerogenic activity profile of a flavonol diglucoside from Equisetum palustre L. J Ethnopharmacol. 2010; 131: 17-21.
Development of self-nanoemulsifying systems containing aceclofenac and evaluation of anti-inflammatory activity in rats
Abstract
Aim: It’s aimed to determine the anti-inflammatory activity of aceclofenac-loaded self-nanoemulsifying systems using carrageenan induced rat paw edema method and to investigate if there was any gastric ulcerogenic activity of the systems with the controlling of petechia in the pylorus.
Materials and Methods: The study was planned as randomized controlled and prospective. The studies were carried out in male, Wistar, albino rats weighing between 200-300 g. Aceclofenac dose given by oral gavage was 10 mg/kg. The study groups were divided into 17 groups (n=6) and each one was administered by oral gavage (0.5 mL sample to 100 g rat). The paw volumes were measured with a plethysmometer at 0th, 90th, 180th, 270th and 360th minutes of administration. Acute toxic effects were investigated and mortality presence was recorded after 48 h. For investigating gastric ulcerogenic effect of aceclofenac, the stomach of the rats were removed and examined for any petechia.
Results: All of the aceclofenac groups, showed maximum edema inhibition at 180th minutes. The value of developed system (ND1+AC), was higher at all the time points compared to other groups (p<0.001) and had no ulcerogenic effect. None of the systems caused petechia dots. There was no acute toxic effect of any groups.
Conclusion: This study indicated that the developed system including aceclofenac was effective and an alternative drug delivery system in medical treatment.
Keywords
Project Number
02/2010-47
References
- 1. Elnaggar YSR, El-Massik MA, Abdallah OY. Self-nanoemulsifying drug delivery systems of tamoxifen citrate: Design and optimization. Int J Pharm. 2009; 380: 133-41.
- 2. Ren F, Jing Q, Cui J, Chen J, Shen Y. Self-nanoemulsifying drug delivery system (SNEDDS) of anethole trithione by combined use of surfactants. J Dispersion Sci Technol. 2009; 30: 664-70.
- 3. Xi J, Chang Q, Chan CK, et al. Formulation development and bioavailability evaluation of a self-nanoemulsified drug delivery system of oleanolic acid. AAPS Pharm Sci Tech. 2009; 10(1): 172-82.
- 4. Shaji J, Lodha S. Response surface methodology for the optimization of celecoxib self-microemulsifying drug delivery system. Indian J Pharm Sci. 2008; 70: 585-90.
- 5. Tang J, Sun J, Cui F, Zhang T, Liu X, He Z. Self-emulsifying drug delivery systems for improving oral absorption of Ginkgo Biloba extracts. Drug Delivery. 2008; 15: 477-84.
- 6. Özbek H, Öztürk A. Antienflamatuvar Etkinliğin Ölçülmesinde Kullanılan Yöntemler. Van Tıp Dergisi. 2003; 10 (1):23-8.
- 7. Ogonowski AA, May SW, Moore AB, et al. Antiinflammatory and analgesic activity of an inhibitor of neuropeptide amidation. J Pharmacol Exp Ther. 1997; 280: 846-53.
- 8. Süleyman H, Demirezer LÖ, Kuruüzüm A, et al. Antiinflammatory effect of the aqueous extract from Rumex patientia L. roots. J. Ethnopharmacol. 1999; 65: 141-8.
- 9. Rimbau V, Cerdan C, Vila R, et al. Antiinflammatory activity of some extracts from plants used in the traditional medicine of North-African countries (II). Phytother Res. 1999; 13: 128-32.
- 10. Vijayakumar CS, Viswanathan S, Reddy MK, et al: Anti-inflammatory activity of usnic acid. Fitoterapia. 2000; 71: 564-6.
- 11. Akkuş Arslan Ş. Kendiliğinden nanoemülsifiye olan ilaç taşıyıcı sistemler. Gazi Üniversitesi / Sağlık Bilimleri Enstitüsü / Farmasötik Teknoloji Ana Bilim Dalı, Doktora tezi, Ankara, Türkiye, 2013.
- 12. Nagda C, Chotai NP, Patel U, et al. Preparation and characterization of spray-dried mucoadhesive microspheres of aceclofenac. Drug Dev Ind Pharm. 2009; 35(10): 1155-66.
- 13. Shaikh IM, Jadhav SI, Jadhav KR, Kadam VJ, Pisal SS. Aceclofenac organogels: In vitro and in vivo characterization. Curr Drug Delivery. 2009; 6: 1-7.
- 14. Yesilada E, Gurbuz I. Evaluation of the antiulcerogenic activity profile of a flavonol diglucoside from Equisetum palustre L. J Ethnopharmacol. 2010; 131: 17-21.
Details
| Primary Language | Turkish |
|---|---|
| Subjects | Health Care Administration |
| Journal Section | Orıgınal Artıcle |
| Authors | |
| Project Number | 02/2010-47 |
| Publication Date | September 27, 2022 |
| Published in Issue | Year 2022 Volume: 13 Issue: 3 |
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e-ISSN: 2149-8296
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