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"Liposomes are used for drug carriers meaning that drugs are incorporated in the membrance or the vesicle of the liposomes. In this study, liposomes were prepared from mixed micelles, consisting of phosphatidylcholone, without or with cholesterol and sodium cholate was added in several ratios namely 0.44; 0.55; 0.63; 0.70; 0.90 and 1.10. After the preparation, the sodium cholate has been removed by a dialysis membrance, using the Hemoflow High Flux, which is generally used for haemodialysis. The Hemoflow High Flux is a tool an effort to obtain a simple, quick, effective method for removing sodium cholate in the process of preparing liposomes. The effectiveness of this tool was proved by the particle size of the liposome which was measured by the Malvern Particle Sizer. The particle size of the liposome consisting of phosphatidycholine (PC) without cholesterol and with cholesterol was 63-68 nm at all ratios andapproximately 125 nm at the ratio of 0.55; 0.63; 0.70, respectively. The particle size of the liposome tended to be smaller after dialyzing although the concentration of lipids tended to increase. However, a larger amount of buffer solution has to be used with this method."

"Pemanfaatan mikrosfer sebagai agen penghantar obat telah banyak dikembangkan. Polipaduan PLLA dan PCL digunakan sebagai bahan dasar pembuatan mikrosfer untuk meningkatkan kemampuan permeabilitas dan laju degradasi dari mikrosfer. Pada penelitian ini mikrosfer polipaduan dibuat dengan memvariasikan konsentrasi surfaktan, kecepatan pengadukan dispersi, dan waktu pengadukan dispersi untuk melihat pengaruhnya terhadap bentuk fisik mikrosfer, persen padatan mikrosfer yang diperoleh, serta ukuran dan keseragaman dari mikrosfer. Mikrosfer yang diperoleh dikarakterisasi dengan FT IR, PSA, dan Mikroskop Stereo. Hasil penelitian menunjukkan bahwa semakin besar konsentrasi surfaktan yang digunakan menghasilkan ukuran mikrosfer yang semakin kecil. Pada variasi kecepatan pengadukan, jika kecepatan pengadukan ditingkatkan diperoleh ukuran mikrosfer yang semakin kecil, namun setelah melewati kondisi optimum kecepatan yang terlampau tinggi mengakibatkan ukuran kembali besar karena meningkatkan kemungkinan mikrosfer yang belum padat untuk bertemu dan menyatu kembali Untuk variasi waktu pengadukan dispersi diperoleh waktu pengadukan paling baik yaitu 1 jam karena menghasilkan mikrosfer dengan ukuran terkecil dan keseragaman yang baik.

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The use of microspheres as drug delivery agents has been widely developed. Polyblend is used as the base material for making microspheres to increase permeability and degradation rates of the microspheres. In this study, the polyblend microspheres were made by varying the surfactant concentration, the dispersion stirring speed, and the time of dispersion stirring to see the effect on the physical shape of the microspheres, the percentage of solid microspheres obtained, the size and uniformity of the microspheres. The microspheres obtained were characterized by FT IR, PSA, and Stereo Microscope.

The results show that the smaller the concentration of surfactants used will result in smaller sizes of microspheres. At variations in stirring speed, if the stirring speed is increased, the smaller the size of the microspheres will be. But after passing the optimum speed, the size of the microspheres will be enlarged again because it increases the possibility of the microspheres that have not been solid to reunite. For variations in the time of dispersion, the best stirring time is obtained 1 hour because it produces microspheres with small size and good uniformity."

"Sebagai suatu pembawa obat (drug carrier), liposom dapat mengubah farmakokinetik obat yang dibawanya, sehingga obat dapat bekerja langsung pada target sasaran sedangkan efek sampingnya akan berkurang. Untuk menjadi pembawa obat yang baik, liposom harus memenuhi persyaratan mutlak yaitu stabil secara kimia, fisika dan biologi. Salah satu faktor yang mempengaruhi kestabilan liposom adalah komposisi penyusunnya, antara lain yang sedang dikembangkan saat ini adalah liposom EPC-TEL 2,5. Liposom EPC-TEL 2,5 tersusun atas Fosfatidilkolin kuning telur (egg-yolk Phosphatidylcholine=EPC) dan Tetraeter lipid (TEL) yang berasal dari bakteri Thermoplasma acidofilum. Dalam penelitian ini akan dilakukan uji stabilitas kimia berupa penambahan garam NaCl 150 mOsmol pH 7 pada liposom EPC-TEL 2,5 yang telah disonikasi selama 60 menit. Penambahan jumlah liposom berukuran lebih dari 100 nm, menjadi indikator perubahan stabilitas liposom pada penelitian ini. Hasil dan Kesimpulan: Tidak terdapat penambahan jumlah liposom yang berukuran lebih dari 100 nm secara bermakna setelah penambahan garam NaCl 150 mOsmol pH 7 dibandingkan kontrol.

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As a drugs carrier, liposome can alter the pharmacokinetics of the entrapped drugs. Thus, drugs can act directly on the targeted cell while their systemic side effects are reduced. To become an effective drugs carrier, liposome must reach its stability in chemical, physical, and biological conditions. Liposome stability can be achieved by changing the lipid composition, such as EPC-TEL 2,5 which is made from the combination of Egg Yolk Phosphatydyl Coline (EPC) and TEL 2,5 mol % that is extracted from Thermoplasma acidofilum. The aim of this study is to test the chemical stability of liposome EPC-TEL 2,5 with sonication by addition of NaCl 150 mOsmol pH 7 solution. The increase in number of liposome larger than 100 nm is the stability parameter in this study. After observation at day 0, 7, 30, 60, 90, there was no significant increase in the number of liposome larger than 100 nm after addition of NaCl 150 mOsmol pH 7 compared with control."

"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."

"Telah dilakukan penelitian untuk menguji stabilitas fisik dan kimia secara in vitro dan stabilitas biologik secara in vivo terhadap formula terbaru liposom EPC-TEL2,5. Liposom sebagai pembawa berbagai obat (drug carrier) yang berukuran 50 - 200 nanometer, merupakan salah satu produk teknologi nano (nanotechnology). Liposom ini merupakan formulasi terbaru yang mengandung lesitin / fosfatidilkolin kuning telur (egg yolk phosphatidyl choline=EPC dan Tetra eter lipid (TEL) 2,5 mol % dari Sulfolobus acidocaldarius atau Thermoplasma acidophilum.yang kemudian dinamakan sebagai liposom EPC-TEL2,5, belum pernah diuji stabilitasnya. Pada penelitian ini digunakan TEL dari Thermoplasma acidophilum. Kestabilan liposom dalam membawa obat hingga mencapai organ sasaran akan sangat menentukan dosis terapi obat. Uji kestabilan liposom EPC-TEL2,5 dilakukan pada liposom tanpa perlakuan (tanpa ekstrusi atau sonikasi), liposom hasil ekstrusi membran 200 nm, dan liposom hasil sonikasi. Secara fisik, uji dilakukan dengan cara mengukur jumlah dan diameter partikel liposom setelah penyimpanan pada suhu 4º C, suhu kamar, dan 37º C. Secara kimia dengan mengukur jumlah dan diameter partikel liposom setelah pemaparan garam NaCl; CaCl2; MgCl2 pada pH 5; 7; 9. Pengukuran jumlah dan diameter partikel liposom ke dua jenis uji stabilitas dilakukan pada hari I; hari VII; akhir bulan I; bulan II, dan bulan III. Secara biologik dilakukan pengukuran hasil degradasi TEL pada menit ke 0; 30; 60; jam ke 2; 4; dan 8 setelah penyuntikan liposom EPC-TEL2,5 secara IP, pada mencit. Hasil uji menunjukkan bahwa liposom tampak stabil hingga akhir bulan I pada suhu 4º C dan 37º C pada uji stabilitas fisik; tetap stabil hingga akhir bulan II pada uji stabilitas kimia pada larutan garam NaCl; CaCl2 pada pH 5 dan 7. Liposom EPC-TEL2,5 terdegradasi di hepar mencit pada uji stabilitas biologik.

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The Physical, Chemical, and the Biological stability test on Liposome EPC-TEL 2.5 as the newest drug delivery systems (drug carrier), in vitro and in vivo. This experiment is carried out in order to improve the stability of the Liposome EPC-TEL 2.5 physically, chemically, and biologically. As a new formula, this liposome that has contained phosphatidylcholine from egg yolk=EPC and Tetra-ether Lipid (TEL) from membrane of Sulfolobus acidocaldarius or Thermoplasma acidophilum had never been tested on their stability. The stability of liposome to carry the drug into the targeted cells or organs is required for determining the therapeutic dose of the drugs. Physically, the test was done by measuring the amount and diameter of liposome after incubating at 4º C, at room temperature, and 37º C. Chemically, the test was also done using the same parameters after introduction of chemical solution of NaCl, CaCl2; MgCl2 at the pH of 5; 7; 9. The measurements was carried out on day 1; 7; and month 1; 2; and 3. Biologically, liposome EPC-TEL 2.5 was injected Intra-Peritoneally to mice to detect the degradation of TEL in their liver, at the minute of 0; 30 ; 60 ; the hour of 2; 4; and 8. The results of these tests were shown that liposome EPC-TEL 2.5 was stable until the last month of 1 at 4º C and 37º C on physical stability test; more stable at the chemical solution of NaCl and CaCl2 at the pH of 5 and 7 until two months; and TEL was degradable in liver of mice."

"Diameter liposom adalah satu dari beberapa parameter untuk menetukan kestabilan liposom sebagai pembawa obat. Namun, banyak masalah yang telah ditemukan dalam pengukurannya seperti alat yang digunakan untuk mengukur diameter liposom (particle seizer) sangat mahal, ukuran liposom yang diukur dengan alat ini memiliki nilai yang bervariasi karena pergerakan Brownian dari liposom. Dalam penelitian sebelumnya, pengukuran diameter liposom hasil sonikasi EPC-TEL 2,5 dengan penambahan larutan CaCl2150 mOsmol pH 7 selama 90 hari yang menggunakan skala Olympus, tidak hanya membutuhkan waktu yang lama, tetapi juga data yang didapatkan hanya dalam skala kategorik. Untuk mengukur diameter liposom secara tepat (kuantitatif), program Image Pro Express 4.5 digunakan pada penelitian ini. Hasil yang didapatkan adalah ukuran ratarata diameter liposom EPC-TEL 2,5 yang termasuk kategori liposom besar (≥100 nm) pada hari ke-0 dan hari ke-90 adalah 112,09 nm dan 121,96 nm; untuk liposom kecil (≤ 100 nm) adalah 73,94 nm dan 66,52 nm.

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The diameter of liposome is one of several parameters to determine the stability of liposome as drug carrier. But, many problems were found in our laboratory to measure it. The problems were the equipment to measure the diameter of liposome that has famous named of particle seizer was too expensive; the size of liposome that has detected with this equipment has many variable values because of the Brownian movement of liposome. In our previous study, measuring the diameter of liposome EPC-TEL 2,5 from sonication with adding of CaCl2 150 mOsmol in pH 7 for 90 days, which has used the Olympus scale, not only time consuming but also the diameter data were the categorical level. To measure the exact diameter of liposome (quantitative), the Image Pro Express 4.5 has used in this experiment. The results were shown that the average size of diameter of big liposome at day 0 and 90 are 112,09 nm and 121,96 nm; for small liposome, the average size of diameter are 73,94 nm and 66,52 nm."

"Latar belakang: Inkorporasi obat ke dalam bahan pembawa obat yaitu liposom dapat menurunkan dosis terapi dan dapat langsung mencapai organ sasaran. Hal ini merupakan upaya penekanan efek samping obat. Tapi, liposom EC-TEL2,5 sebagai formula baru belum pernah diuji stabilitas secara fisik. Tujuan: Menguji stabilitas fisik liposom EPC-TEL2,5 hasil sonikasi dan ekstrusi dibandingkan dengan kontrol pada suhu penyimpanan 4oC. Metode: Penelitian dilakukan dengan metode eksperimental in vitro pada tiga kelompok liposom, yaitu kelompok ekstrusi 200 nm, kelompok sonikasi dan kelompok kontrol. Pengamatan terhadap sediaan liposom dilakukan pada hari ke-0, hari ke-7, hari ke-28, hari ke-56 dan hari ke-84. Hasil pengamatan dikategorikan menjadi dua, yaitu liposom dengan diameter < 100 nm dan diameter > 100 nm. Hasil: Hasil uji statistik Kruskall-Wallis dan analisis post hoc Mann-Whitney didapatkan nilai probabilitas 0,935 (p=0,935) untuk liposom hasil sonikasi dengan kategori diameter < 100 nm, sedangkan nilai probabilitas untuk liposom hasil sonikasi dengan kategori diameter > 100 nm adalah 0,242 (p=0,242 ). Nilai probabilitas untuk liposom hasil ekstrusi dengan diameter < 100 nm adalah 0,007 (p=0,007), sedangkan nilai probabilitas untuk liposom hasil ekstrusi dengan kategori diameter > 100 nm adalah 0,008 (p=0,008). Kesimpulan: Liposom EPC-TEL2,5 hasil sonikasi yang disimpan ada suhu 4oC selama 84 hari bersifat stabil secara fisik, sedangkan hasil ekstrusi yang disimpan ada suhu 4oC selama 84 hari bersifat tidak stabil secara fisik dibandingkan dengan kelompok kontrol.

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Background: Incorporation of drug in drug vehicle, liposome, can lower drug concentration within therapeutic dose and can arrive at target organ directly. This is one way to suppress side effect of drugs. But, liposome EPC-TEL2,5 as new formula has not been tested for physical stability. Objective: To test the physical stability of liposome EPC-TEL2,5 prepared by extrusion, sonication compared to control at incubation temperature 4oC. Methods: This research is experimental study (in vitro) in three groups of liposomes, they are 200 nm-extrusion group, sonication group and control group. Observation to all groups of liposomes were done in 0 day, 7th day, 28th day, 56th day and 84th day. The result of this observation is the amount of liposomes categorized in two groups, they are liposomes with diameter > 100 nm and liposomes with diameter < 100 nm. Result: Post hoc analysis with Mann-Whitney test showed that the probability value is 0,935 (p=0,935) for liposomes as result of sonication with diameter ≤ 100 nm, and the probability value for liposomes as result of sonication with diameter > 100 nm is 0,242 (p=0,242). The probability value of liposomes as result of extrusion with diameter < 100 nm is 0,007 (p=0,007), and the probability value for liposomes as result of extrusion with diameter > 100 nm is 0,008 (p=0,008). Conclusion: Liposomes EPC-TEL 2,5 as result of sonication which have been incubated at 4oC for 84 days were physically stable and extrusion incubated at 4oC for 84 days were physically unstable compared to control group."

"Sebagai pembawa obat yang langsung bekerja pada sel target, liposom terbukti meningkatkan efektivitas obat dan mengurangi efek samping sistemik, terutama untuk terapi jangka panjang. Liposom yang saat ini sedang dikembangkan, merupakan kombinasi fosfatidil kolin kuning telur (Egg yolk Phosphatidil Choline / EPC) dan Tetraeter Lipid 2,5 mol % dari Thermoplasma acidophilum yang kemudian dinamakan sebagai liposom EPC-TEL 2,5. Penelitian ini bertujuan untuk menguji kestabilan liposom EPC TEL 2,5 hasil sonikasi selama 60 menit, dalam larutan garam yang lazim digunakan sebagai larutan elektrolit, NaCl dan CaCl2 pH 7, dengan penyimpanan pada suhu 4oC dan pengamatan pada hari ke-0, 7, 30, 60, dan 90. Parameter kestabilan yang diukur adalah tidak bertambahnya diameter liposom dan jumlah liposom yang berukuran lebih dari 100 nm. Hasil dan Kesimpulan: Tidak terjadi peningkatan jumlah liposom yang berukuran lebih dari 100 nm secara bermakna pada liposom yang terpapar NaCl 150 mOsmol pH 7 maupun CaCl2 150 mOsmol pH 7.

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Comparative Stability Test of Liposome Tetraether Lipid (EPC-TEL 2,5) After Sonication in NaCl 150 mOsmol pH 7 and CaCl2 150 mOsmol pH 7 Solutions. As a drug carrier which is directly act on targeted cell, liposome has proved to increase drug efficacy and reduce systemic side effect of drugs, especially for long term therapy. Liposome, which has still developed, is the combination of Egg yolk Phosphatidyl Choline (EPC) and Tetraether Lipid 2,5 mol % isolated from the archaebacterium Thermoplasma acidophilum, which is called EPC-TEL 2,5. The aim of this study is to prove the chemical stability of liposome EPC-TEL 2,5 with the addition of selected salts which are commonly used as electrolyte solution (NaCl pH 7 dan CaCl2 pH 7 150 mOsmol), after 60 minutes sonication and storage in 4oC, after observation at day 0, 7, 30, 60, 90. The stability parameters in this study are that diameter of liposome and the amount of liposome larger than 100 nm. There was no significant different between the amount of liposome which have sizes greater than 100 nm in addition of NaCl 150 mOsmol pH 7 or CaCl2."