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"Penelitian ini dilakukan untuk menganalisis distribusi liposomal-metilprednisolon palmitat (L-MPLP) di beberapa organ pada mencit C3H setelah pemberian secara intra-peritoneal. Sebagai formula baru, L-MPLP pada membran liposom meningkat dari 70% menjadi 95% setelah digunakan tetra eter lipid dalam komposisi liposom sebagai penstabil membran. Atas dasar penelitian tersebut, L-MPLP akan terdistribusi dengan lebih baik di beberapa organ pada mencit dibandingkan control yaitu MPLP sebagai obat bebas, metilprednisolon (MPL) sebagai standar dan liposom tanpa obat. Empat puluh dua mencit C3H dibagi ke dalam 5 grup penelitian. Setiap grup dibagi ke dalam 6 waktu penelitian. Setiap obat disuntikkan intra-peritoneal. Darah diambil dari vena ekor (menit ke 10; 30; 60; 90; 180 dan jam ke 48) dan dilakukan ekstirpasi organ (hepar, limpa, timus, ginjal dan sumsum tulang) pada menit ke setalah mencit dimatikan dengan eter. Distribusi L-MPLP dalam organ tampak jelas pada menit ke 180 dan menurun setelah 48 jam. Distribusi obat atau metabolitnya tampak menonjol pada hepar, diikuti secara berurutan oleh limpa, timus, ginjal dan sumsum tulang.

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The Distribution of Liposomal-Methylprednisolone Palmitate (L-MPLP) in Several Organs in Mice after Intra-Peritoneal Injection. This study was to analyze the distribution of liposomal-methylprednisolone palmitate (L-MPLP) as a new drug formulation, in several organs of mice after intra-peritoneal injection. In a previous study, in vitro, the stability and the incorporation of methylprednisolone palmitate into liposome membranes were increased, from 70% to approximately 95% using tetra-ether lipid as a stabilizer of the liposome membrane. Based on this result, the stability of L-MPLP should also be proved, in vivo, that the drug, methylprednisolone palmitate, could be distributed into several organs more effective than in a control group (methylprednisolone palmitate and methylprednisolone as a standard of drug and liposome). Forty-two mice of C3H were divided into 5 study groups. Each group of animals was divided into 6 sub-groups of time from 10 minutes to 48 hours. Each drug was injected intra-peritoneal, blood was drawn from the vein of the tail and the organs i.e. liver, kidneys, spleen, thymus, and bone marrow were extirpated after sacrificing the mice using ether. The distribution of the drug or their metabolites was higher at the minute of 180 and tended to decrease at the time of 48 hours after injection. The higher distribution was shown in the liver and rather high in the spleen, thymus, kidney, and bone-marrow respectively."

"This study is proposed to solve the main problem in the first experiment which has the pitfall of the incorporation of methylprednisolone (MPL) into liposome's membrane. The liposomal-methylprednisolone (L-MPL) has already been formulated by Mishina, et at31.32 and experimented on several studies of organ transplantation in rat, successfully. But, all procedures even using other combination and ratio of lipids are irreproducible methods. The pitfall of the incorporation of MPL into liposome's membrane is caused by the micelle formation of MPL.To reduce or may be to inhibit the micelle formation of MPL that usually formed spontaneously when it is dispersed in aqueous media, the reactive -OH group at C21 position should have been esterified with palmitate to enhance the lipophilicity of the drug. This reaction, based on the Benameur's method, yielded 71% of pure methylprednisolonepalmitate (MPLP) as a new drug. To analyze the properties of this drug such as the stability or the availability of the drug both in liposome's membrane and in several organs in vivo, several studies have already been done in this study using sophisticated equipment.The incorporation of the new drug , MPLP, into liposome's membrane of a conventional liposome of Egg-yolk Phosphatidylcholine (EPC) was 70 %_ The incorporation was increased to approximately 95 % in liposome's membrane of EPC and tetra ether lipids (TEL) from Sulfolobus acidocaldarius as a stabilizer of the liposomal membrane The newest drug that is proposed in evaluating the stability of the drug in vitro and the distribution of the drug on several organs in mice is liposomal- methylprednisolone-palmitate (L-MPLP).The stability of L-MPLP in vitro was evaluated on their particle size. They were more stable at 20° C for 9 days of incubation than at room temperature. In vivo study of L-MPLP were shown as a distribution of the metabolite of MPL or MPLP on several organs on TLC where the distribution in the liver has more higher than in the spleen, kidney, thymus, and bone-marrow, in sequence. The distribution of the metabolite of L-MPLP in the liver has also shown higher than the metabolite of the control group of liposome, MPL, or MPLP as a free drug.Because of these successful results, this experiment will have to be continued to improve the stability of this drug and to analyze the other effects on immunosuppressive properties, toxicity, pharmacokinetics and pharmacodynamics of the drug."

"Ruang lingkup dan metodologi: Glukokortikoid telah lama digunakan sebagai antiiflamasi dan imunosuppresan. Penggunaan yang panjang dengan dosis tinggi menyebabkan efek samping yang cukup serius. Dewasa ini telah dikembangkan berbagai pembawa obat yang dapat membawa obat langsung ke target obat atau ke reseptornya. Dengan menginkorporasikan obat ke pembawa obat, contohnya liposom, efek samping sistemik dapat ditekan. Purwaningsih dkk telah berhasil membuat sediaan baru yakni Liposom-metilprednisolon palmitat (L-MPLP). Penelitian ini bertujuan untuk mempelajari efek farmakologi dari L-MPLP, terutama efek antiinflamasinya. Parameter yang dilihat adalah penurunan produksi interferon gamma pada kultur limfosit T setelah distimulasi dengan concanavalin A secara in vitro maupun in vivo. Hasil dan Kesimpulan : Terjadi penurunan kadar interferon gamma setelah pemberian L-MPLP secara in vivo pada dosis 2, 8 dan 16 mg/kgBB secara signifikan dibandingkan kontrol tanpa perlakuan sedangkan pemberian MPL tidak terjadi penurunan kadar interferon gamma. Pada kultur in vitro, pemberian L-MPLP maupun MPL pada kadar 5.10 -1, 5.10-2 dan 5.10-3 keduanya mampu menekan produksi interferon gamma, dimana penekanan oleh L-MPLP lebih baik dibanding MPL secara signifikan.

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The Improving of Methylprednisolone Palmitate Potency After Incorporated With Liposome. An Antiinflammation Study In Culture Of Mice?s Splenocytes. Glucocorticoid has been used as an antiinflammatory and immuno-suppresive drug. Longterm utilisation at high dose of glucocorticoid is associated with serious side effects. In recent years, many attempts have been performed in searching the appropiate vehicles to deliver the drug directly into the target organ or the receptor. By incorporating the drug into its vehicle such as liposome, the systemic side effect can be minimized. Purwaningsih et al has successfully synthetized a novel preparation of liposome methylprednisolone palmitate (L-MPLP). The aim of the study was to learn the pharmacological effect of L-MPLP, especially on antiinflammatory effect of this novel preparation, compared with the standard methylprednisolone (MPL). The parameter was the potency of L-MPLP in reducing gamma-interferon production in T-lymphocyte culture after stimulation with concanavalin A in vitro as well as in vivo. Gamma-interferon was assayed by ELISA method. The reduction of gamma interferon, in vivo, after the administration of L-MPLP at the dose of 2,8 and 16 mg/kgBW respectively, showed significant difference than a control group, while MPL did not. The addition of both L-MPLP and MPL in in vitro culture at the concentration of 5.10-3, 5.10-2 and 5.10-1 mM have proved to suppress the gamma-interferon production, where the suppression of L-MPLP was more effective than MPL, significantly."

"Liposom sebagai sistem penghantaran obat dapat mengurangi efek samping dan toksisitas obat karena membantu menargetkan obat ke targetnya secara spesifik. Pada daerah yang terinfeksi biasanya bersifat asam, oleh karena itu perlu dibuat liposom sensitif pH. Tujuan dari penelitian ini adalah untuk mengetahui pengaruh penambahan asam palmitat terhadap sensitivitas liposom yang mengandung spiramisin pada berbagai kondisi pH dan mengevaluasi kemampuan penjerapannya. Pada penelitian ini dibuat tiga formulasi yaitu tanpa penambahan asam palmitat, dengan penambahan satu mol asam palmitat dan penambahan dua mol asam palmitat. Liposom dievaluasi bentuk dan morfologinya menggunakan Scanning Electron Microscope (SEM) serta diamati distribusi ukuran partikelnya dengan Particle Size Analyzer (PSA), persentase penjerapan yang diperoleh dari hasil ultrasentrifugasi dan yang utama adalah sensitivitas liposom pada pH 2; pH 5,5; dan pH 8. Hasil yang didapat adalah liposom dengan rentang diameter 100-200 nm dan efisiensi penjerapan dari ketiga formula menurun dengan meningkatnya konsentrasi asam palmitat. Efisiensi penjerapan dari ketiga formula menurun dengan meningkatnya konsentrasi asam palmitat. Kemampuan penjerapan liposom sensitif pH yaitu 82,22% dan 81,94%. Pelepasan obat tertinggi didapat pada liposom medium pH 2 dan terendah pada medium pH 8.

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Liposomes as drug carrier in order to reduce adverse effects and toxicity of drugs because applied for drug targetting specificly. In the infection area usually in acidic condition so it is so important to make pH sensitive liposome. The aims of this research are to study about the presence of palmitic acid in liposome formula containing spiramycin on their pH sensitivity and to evaluate their entrapping efficiency. There are three concentrations of palmitic acid that use in liposome formula which are 1 mol, and 2 mol. Liposomes were evaluated by their morphology with Scanning Electron Microscopy (SEM), particle size distribution with Particle Size Analyzer (PSA), entrapment efficiency with ultracentrifugation, and their sensitivity in pH 2; 5.5; and 8 medium. Evaluation results showed that liposomes particle sizes are range from 100-200 nm, and it illustrated that the higher palmitic acid concentration gave the lower their entrapment efficiency. The pH sensitive liposome has entrapment efficiency 82.22% and 81.94%. The highest drug released could be obtained from liposomes in pH 2 medium while the lowest drug released was in pH 8 medium."

"Liposom merupakan salah satu produk nanoteknologi yang sedang dikembangkan untuk meningkatkan efektivitas dan mengurangi efek samping obat. Sebagai pembawa obat, kini telah dikembangkan liposom EPC-TEL 2,5, yang mengandung fosfatidilkolin kuning telur (egg yolk phosphatidyl choline = EPC) dan TEL 2,5 mol%. Belum banyak penelitian tentang stabilitas liposom yang mengandung TEL ini. Pengukuran diameter, salah satu parameter stabilitas liposom, selama ini dilakukan menggunakan particle sizer, yang harganya mahal dan tidak selalu tersedia. Alternatif yang sedang dikembangkan adalah menggunakan program komputer Image pro Express. Penelitian ini membandingkan diameter liposom EPC-TEL 2,5 hasil sonikasi, yang diukur dengan program Image pro Express, sebelum dan sesudah paparan larutan CaCl2 150 mOsmol pH 5 selama penyimpanan 90 hari pada suhu 4oC. Berdasarkan penelitian, terdapat perbedaan bermakna dengan p = 0.001 antara diameter liposom EPC-TEL 2,5 hasil sonikasi sebelum dan sesudah paparan larutan CaCl2 150 mOsmol pH 5 selama penyimpanan 90 hari.

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Liposome is a nanotechnology products which is being currently developed to improve the effectiveness and reduce the side effect of a drug. Presently, liposome EPC-TEL 2.5, which contains egg yolk phosphatidylcholine (EPC) and tetra-ether lipid (TEL) 2.5 mol%, has been developed to act out as a drug carrier. These days, researches on TEL containing liposome are still rare. Today, diameter measurement, one of the liposome stability parameter, is still performed by using particle sizer, which are expensive and not always available. One alternative that has been being developed is the application of Image pro Express computer program. This research compares the diameter of a sonicated liposome EPC-TEL 2.5, which measured using Image pro Express, before and after exposure to CaCl2 150 mOsmol pH 5 solution for 90 days at 4oC. Based on the research, there is statistically significant difference (p = 0.001) in diameter of sonicated liposome EPC-TEL 2.5, before and after exposure to CaCl2 solution (150 mOsmol at the pH of 5) in a 90 days incubation."

"Liposom merupakan sistem penghantaran obat nanopartikel berbasis lipid yang bersifat biokompatibel dengan berbagai obat, peptida, protein, dan plasmid DNA. Dalam menghasilkan liposom yang berukuran 0,1-1 μm diperlukan metode yang tepat sesuai karakteristik yang diinginkan. Metode ekstrusi secara bertingkat akan mengecilkan ukuran partikel liposom dengan hasil yang lebih homogen. Penelitian ini dilakukan untuk membuat dan mengkarakterisasi liposom spiramisin yang ditambahkan asam palmitat dan diperkecil ukurannya dengan ekstrusi bertingkat. Liposom dibuat dengan metode hidrasi lapis tipis dan dilanjutkan dengan ekstrusi bertingkat melalui membran polikarbonat 0,4 μm dan 0,2 μm. Penggunaan asam palmitat pada formulasi liposom diharapkan dapat menambahkan sifat fleksibilitas saat liposom diekstrusi melalui membran berpori. Pada penelitian ini digunakan spiramisin untuk mempelajari kemampuan penjerapan liposom. Berdasarkan evaluasi diperoleh liposom multilamela dengan efisiensi penjerapan yang menurun setelah diekstrusi yaitu 87,98 ± 0,73%, 48,15 ± 4,01%, dan 28,35 ± 1,18%. Hasil ekstrusi juga menunjukkan ukuran diameter partikel rata-rata yang menurun sebesar 536, 408, dan 403 nm. Hasil analisa termal menunjukkan asam palmitat sedikit meningkatkan sifat rigiditas dari liposom sehingga mampu menaikkan kemampuan penjerapan liposom spiramisin

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Liposomes as drug delivery system are lipid-based nanoparticles that are biocompatible with various drugs, peptides, proteins, and plasmic DNA. The appropriate methods are needed in producing liposomes which the size is 0.1 up to 1 μm according to the desired characteristics. The sequential extrusion is a method that is able to shrink the particle size of liposome with a more homogeneous results. The aim of this study is to make and characterize a liposome that entrap spiramycin in addition of palmitic acid which is reduction of particle size with sequential extrusion method. Liposomes were prepared by thin-layer hydration followed by sequential extrusion through a polycarbonate membrane 0.4 μm and 0.2 μm. Palmitic acid in liposome formulations are expected to add flexibility properties as liposomes extruded through a porous membrane. In this study spiramycin used to study the entrapment ability of liposomes. Based on the evaluation, multilamela liposomes was obtained and the entrapment efficiency were 87.98 ± 0.73% with decreased after extruded, 48.15 ± 4.01%, and 28.35 ± 1.18%, respectively. Extrusion also indicate the average of particle size is decreased by 536, 408, and 403 nm. Thermal analysis results showed palmitic acid slightly increases the rigidity properties of the liposomes so that can increase the ability of entrapment."

"Dalam formulasi obat, pembawa obat (drug carrier) memegang peranan penting karena diharapkan dapat meningkatkan efektivitas obat dan keamanan. Di lain pihak, dapat menurunkan efek samping bila digunakan dalam waktu lama. Salah satu bahan pembawa obat yang sedang dikembangkan akhir-akhir ini adalah liposom. Liposom dengan formulasi EPCTEL 2,5 yang berasal dari fosfatidilkolin kuning telur dan Tetra Eter Lipid 2,5 mol % telah terbukti menunjukkan distribusi dalam organ yang lebih baik.2 Akan tetapi, stabilitas liposom tersebut secara kimia belum pernah diuji. Penelitian ini bertujuan untuk menguji stabilitas liposom EPC-TEL 2,5 yang telah disonikasi dan diberikan larutan MgCl2 350 mOsmol pH 7. Parameter yang dilihat adalah ukuran diameter liposom ≤100 nm dan >100 nm. Liposom dikatakan stabil bila ukuran diameter tidak berubah jumlahnya setelah pemaparan larutan MgCl2 dari waktu ke waktu. Hasil dan kesimpulan yang didapatkan pada uji ini adalah jumlah liposom sonikasi tidak stabil pada diameter ≤100 sampai akhir penelitian. Sedangkan jumlah liposom pada diameter >100 tidak dilakukan perhitungan analisis data karena data jumlah liposom diameter >100 pada hari ke-0 tidak ada.1-3

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Stability Test of Sonication Liposome Tetra Eter Lipid (EPC-TEL 2,5) with MgCL2 350 mOsmol PH 7 Exposure at 40 Celcius. Drug delivery in drug formulation have an important role because it will increase drugs effectivity and safety. On the other side, also decrease drug’s side effect if it is used for a long time. Recently, one of drug carrier products which is developed is liposome. Liposome with EPC-TEL 2,5 formulation from egg-yolk phosphatidylcholine and Tetra Eter Lipid 2,5 mol % has been proved to show better distribution in organs.2 But, the stability of liposome is never tested chemically. This research main purpose is to test liposome EPC-TEL 2,5 stability after it given sonication and exposed with MgCL2 350 mOsmol pH 7. The object to analyze is only liposome with ≤ 100 nm and > 100 nm diameter. It will be clasified as stable if the diameter doesn’t change after exposed with MgCL2 from time to time. The result and conclusion from this test is the amounts of sonication liposome isn’t stable in diameter ≤ 100 until the end of researching. While, the amounts of sonication liposome in diameter > 100 wasn’t counted data analysis because there is nothing the amounts of liposome diameter >100 at the first researching.1-3"

"Tomato (Solanum lycopersycum L.) that the fruit mainly contained lycopene, beta carotene, vitamin C and vitamin E indECated that the fruit had antioxidant activity. These compound were known able to prevent and retention of free radECal forming whECh can cause aging and chronEC disease. This research, tomato with different concentration 0,5%, 1%, 2%, and 3% were formulated in cream. PhysECal stability test including the storage at three different temperatures including cool temperature (4°C), room temperature, and high temperature (40+2°C), mechanECal test, and cycling test. Measurement of antioxidant activity tomato cream that using DPPH method pursuant to value of DPPH retention (EC50). This research resulted that shown tomato cream 0,5% 1%, 2%, and 3% have physECal stability with storage at cool temperature (4oC), room temperature, and high temperature (40+2°C). Tomato cream 1%, 2%, and 3% reach minimum value of retention DPPH (EC50) but tomato cream 0,5% not reach minimum value of retention DPPH (EC50). Cream tomato 1% have the best physECal stability and cream tomato extract 3% have the best antioxidant activity."

"Telah dilakukan pengujian pengaruh suspensi ekstrak tribulus (Tribulus cistoides) dosis 400, 800, 1600, dan 3200 mg/kg bb selama 3 hari terhadap mencit jantan yang sebelumnya ielah diberi asetaminophen dosis 140 mg/kg bb/ hari selama 30 hari berturut-turut. Hasil uji stastistik terhadap parameter-parameter lalensi penunggangan, latensi intromisi, latensi ejakulasi, jumlah penunggangan, dan jumlah tntromtsi menunjukkan adanya perbedaan yang nyata (a < 0,05) dibandingkan dengan kontrol. Dengan demikian dapal disimpulkan bahwa pemberian ekstrak tribulus dosis 400, 800, 1600, dan 3200 mg/kg bb selama tiga hari dapat meningkatkan libido mencit, semakin tinggi dosis maka semakin besar libido yang dihasilkan.

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The effect of varying doses (400, 800, 1600, 3200 mg/kg body weight) of tribulus (Tribulus cistoides) extract suspension on libido of male mice for 3 days was investigated. Before treatment, the male mice were previously subjected with 140 mg/kg body weight of acetaminophen for 30 days. The statistical test on mount latency, intromtion latency, ejaculation latency, amount of mounts and amount of intromtions of the male showed significantly difference ( a < 0.05) compared with control. Notably, there was an increase in the male mice libido with increase in concentration of the tribulus extract."