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Abstrak :
Pada penelitian ini nanopartikel verapamil hidroklorida dari kitosan dan natrium tripolifosfat melalui proses gelasi ionik dipreparasi, dikarakterisasi, dan dievaluasi secara in vitro dan in vivo untuk penghantaran transdermal sebagai sediaan antihipertensi. Hasil menunjukkan nanopartikel kitosan-tripolifosfat dapat digunakan. Formula D merupakan formula terpilih yang menghasilkan nanopartikel berukuran 62,8 nm, persen efisiensi penjerapan 59,15 %, potensial zeta +25,46 mV, sferis, dan dapat dikonfirmasi dengan FT-IR. Formula ini selanjutnya digunakan pada pembuatan sediaan. Uji penetrasi secara in vitro yang menggunakan sel difusi Franz menunjukkan sediaan gel nanopartikel dengan propilen glikol sebagai peningkat penetrasi memiliki daya penetrasi terbesar dibandingkan dengan gel nanopartikel tanpa peningkat penetrasi dan pembanding dengan fluks secara berturut-turut adalah 148,33 ± 1,17 μg/cm2.jam; 121,88 ± 0,37 μg/cm2.jam; dan 60,93 ± 0,47 μg/cm2.jam. Uji tekanan darah secara in vivo menggunakan tikus jantan Sprague Dawley menunjukkan sediaan gel nanopartikel dengan peningkat penetrasi memiliki efektivitas penurunan tekanan darah sistolik tertinggi daripada gel nanopartikel secara berturut-turut adalah 14,89% dan 5,87%; efektivitas dalam menurunkan tekanan darah diastolik menunjukkan hasil efektivitas tertinggi pada gel nanopartikel saja sebesar 4,18%; dan efektivitas penurunan tekanan darah arteri rata-rata didapatkan hasil yang sama pada gel nanopartikel dan gel nanopartikel dengan peningkat penetrasi yaitu sebesar 20,61%, semuanya dibandingkan dengan gel pembanding.

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In this research, verapamil hydrochloride nanoparticle from chitosan and sodium tripolyphosphate using ionic gelation method had been prepared, charaterized, and evaluated in vitro and in vivo for antihipertensive transdermal delivery. The results showed that chitosan-tripolyphosphate nanoparticle could be used. The chosen formula was formula D which has 62.8 nm nanoparticles size, 59.15% entrapment efficiency, +25.46 mV zeta potential, spherical, and confirmed with FT-IR. This formula was made into gel dosage form. In vitro penetration test using Franz diffusion cell showed that nanogel with propylen glicol as an enhancer had the greatest penetration result compared to nanogel without enhancher and standard gel with flux were 148.33 ± 1.17 μg/cm2.hours; 121.88 ± 0.37 μg/cm2.hours; and 60.93 ± 0.47 μg/cm2.hours, respectively. In vivo blood pressure test using Sprague Dawley male rats showed nanogel with enhancher has the highest systolic blood pressure reduction than nanogel were 14.89% and 5.87%, respectively; in lowering diastolic blood pressure showed the highest effectiveness of nanogel amounting to 4.18%; and the same effectiveness of mean arterial blood pressure obtained on nanogel and nanogel with enhancer which equal to 20.61%, all compared to the standard gel.

Abstrak :
Kurkumin telah banyak digunakan dan masih terus diteliti pada pemakaian topikal karena mempunyai aktivitas sebagai antioksidan dan antiinflamasi. Pada dasarnya untuk mendapatkan efek yang optimal dari sediaan topikal, zat berkhasiat yang ada dapat terpenetrasi melalui lapisan kulit teratas. Oleh karena itu, dibuat tiga bentuk sediaan guna membandingkan perbedaan jumlah kurkumin yang terpenetrasi, yaitu krim, salep, dan gel. Daya penetrasinya diuji secara in vitro dengan alat sel difusi Franz menggunakan membran abdomen tikus galur Sprague-Dawley. Jumlah kumulatif kurkumin yang terpenetrasi dari sediaan salep, krim, dan gel secara berturut-turut adalah sebanyak 192,22 ± 2,25 μg/cm², 69,18 ± 2,79 μg/cm², dan 32,26 ± 4,63 μg/cm². Persentase jumlah kurkumin yang terpenetrasi dari sediaan salep, krim, dan gel secara berturut-turut adalah 0,53 ± 0,01%, 0,20 ± 0,01%, dan 0,09 ± 0,01%. Selain itu juga dilakukan uji stabilitas fisik melalui cycling test, uji mekanik dan pengamatan pada penyimpanan selama 8 minggu di suhu kamar, suhu hangat (40° ± 2°C), dan suhu dingin (4° ± 2°C). Ketiga sediaan menunjukkan kestabilan fisik dengan parameter kestabilan di ketiga suhu yaitu organoleptis, pH, diameter globul rata-rata, dan konsistensi. ......Curcumin has been used and still being researched in topical use because it has antioxidant and antiinflammation activities. Basically, to get the optimum effect from topical preparation, drug should be penetrated through top skin layer. Therefore, three kinds of preparation were made to measure the total cumulative penetration of curcumin, i.e. cream, ointment, and gel. Penetration ability through skin was examined by in vitro Franz diffusion cell test using Sprague-Dawley rat abdomen skin as membrane diffusion. Total cumulative penetration of curcumin from ointment, cream, and gel preparations measured were 192.22 ± 2.25 μg/cm², 69.18 ± 2.79 μg/cm², and 32.26 ± 4.63 μg/cm², respectively. The percentage of penetrated curcumin from ointment, cream and gel preparations were 0.53 ± 0.01%, 0.20 ± 0.01%, and 0.09 ± 0.01%, respectively. Besides that, it also done stability test including cycling test, mechanical test, and the storage for eight weeks at room temperature, warm temperature (40° ± 2°C), and cold temperature (4° ± 2°C). The three dosage forms showed physical stability w ith stability parameters in the three temperatures were organoleptic observation, pH, globule diameter, and consistency.

Abstrak :
Nanoparticles is one type of drug delivery system which intended to improve the bioavailability of drugs. Nanoparticles can be prepared by several methods and the ionic gelation method is the easiest one. Verapamilhydrochloride is adrugwhich used asantiarrhythmic,antiangina, and antihypertension therapy. Nevertheless, bioavailability of orally administered verapamil is very low, only about 10 to 23%. Therefore, verapamil hydrochloride was prepared as nanoparticlesdosage form to increase its bioavailability. The purpose of the present study was to optimize ionic gelation method of chitosan and sodium tripolyphosphate to obtain thebest nanoparticles formulation. Nanoparticles were obtained from four different methods. Formula A, B and C were produced by drop the sodium tripolyphosphate solution into chitosan solution at 0.75 mL/minute, while formula D were prepared by pour sodium tripolyphosphate solution into chitosan solution. Formula A and B were then strired at 400 rpm, while formula C and D at 3000 rpm. Three grams of verapamil hydrochloride was added into formula A, while formula B, C, and D were produced by adding 5 grams of verapamil hydrocloride. Particle size distribution, zeta potential, entrapment efficiency, morphology, and fourier transform infra red spectrum of each nanoparticles formula were characterized. The chosen formula was formula D which has 62.8 nm of size, 59.15% of entrapment efficiency, +25.46 mV of zeta potential, spherical shape, and the ionic interaction was confirmed by FT-IR spectrum. The results showed that chitosan-tripolyphosphate succesfully produce the verapamil hydrochloride nanoparticles by ionic gelation method.

Abstrak :
Nanopartikel dapat dibuat dengan menggunakan beberapa metode dan metode gelasi ionik adalah yang termudah. Verapamil hidroklorida adalah obat yang digunakan sebagai antiaritmia, antiangina, dan terapi antihipertensi. Namun demikian, bioavailabilitas dari verapamil yang diberikan secara oral sangat rendah, hanya sekitar 10 hingga 23%. Oleh karena itu, verapamil hidroklorida ini dibuat sebagai sediaan nanopartikel untuk meningkatkan bioavailabilitasnya. Tujuan dari penelitian ini adalah untuk mengoptimalkan metode gelasi ionik antara kitosan dan natrium tripolifosfat guna mendapatkan formulasi nanopartikel terbaik. Nanopartikel diperoleh dari empat metode yang berbeda (formula A, B, C, dan D). Distribusi ukuran partikel, potensial zeta, efisiensi penjerapan, morfologi, dan spektrum FT-IR dari nanopartikel dikarakterisasi. Formula yang dipilih adalah formula D yang memiliki ukuran 62,8 nm, efisiensi penjerapan 59,15%, potensial zeta 25,46 mV, bentuk bulat, dan memiliki spektrum FT-IR yang sesuai. Hasil penelitian menunjukkan bahwa kitosan-tripolifosfat dapat menghasilkan nanopartikel verapamil hidroklorida dengan menggunakan metode gelasi ionik.

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Nanoparticles can be prepared by several methods and the ionic gelation method is the easiest one. Verapamil hydrochloride is a drug which used as antiarrhythmic, antiangina, and antihypertension therapy. Nevertheless, bioavailability of orally administered verapamil is very low, only about 10 to 23%. Therefore, verapamil hydrochloride was prepared as nanoparticles dosage form to increase its bioavailability. The purpose of the present study was to optimize ionic gelation method of chitosan and sodium tripolyphosphate to obtain the best nanoparticles formulation. Nanoparticles were obtained from four different methods (formula A, B, C, and D). Particle size distribution, zeta potential, entrapment efficiency, morphology, and fourier transform infra red spectrum of each nanoparticles formula were characterized. The chosen formula was formula D which has 62.8 nm of size, 59.15% of entrapment efficiency, +25.46 mV of zeta potential, spherical shape, and the ionic interaction was confirmed by FT-IR spectrum. The results showed that chitosan-tripolyphosphate succesfully produce the verapamil hydrochloride nanoparticles by ionic gelation method.