1989 – Volume 14, Issue 1

CONTENTS

BİLİMSEL ARAŞTIRMALAR

Kafein ve Parasetamolün Farmasötik Prepara Harda Birinci Türev UV Spektrofometrisi He Miktar Tayinleri

Feyyaz ONUR (*) Nevin ACAR (*)

(*) AÜ. Eczacılık Fakültesi, Analitik Kimya Anabiliın Dalı, Tandoğan.

Pages, 1-7. Abstract | PDF (464KB)

Bazı Solvanlann Antimikrobial Etkileri Üzerinde Bir Çalışma

Ufuk ABBASOĞLU (*)

(*) : G.Ü. Eczacılık Fakültesi, Mikrobiyoloji Bilimdalı

Pages, 9-12. Abstract | PDF (316KB)

Bazı 2-Asetilnaftalen ve p-Kloroasetilbenzen Türevlerinin Oksim ve Redüksiyon Ürünleri Üzeri· Çahşmalar

Fiigeıı ÖZKANU (*) Sevim DALKARA (*) Mevliil ERTAN (*)

(*) H.Ü. Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, Hacettepe~ ANKARA

Pages, 13-22. Abstract | PDF (712KB)

BİLİMSEL TARAMALAR

Selenyum’un İnsan Sağhğındaki Rolü

Filiz HINCAL (*) Nursere11 ATA ÇERİ (*)

(*) H.Ü, Eczacılık Fakültesi, Farmasötik Toksikoloji Anabilirn Dalı, Hacettepe,

Pages, 23-38. Abstract | PDF (1416KB)

İmidazo ( 4,5-b) ve ( 4, 5- c )Piri din Türevleri Ü zerinde Yapılan Yapı-Etki İlişkisi Çalışmaları – I

Doç. Dr. Fatma Gümüş (*)

(*) O.Ü. Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı

Pages, 39-50. Abstract | PDF (1000KB)

Aspirin

Figen OCAK (*) llbeyi AGABEYoGLU (*)

(*) Gazi Üniversitesi Ecz. Fak., Eczacılık Teknolojisi Bölümü, Ankara.

Pages, 51-63. | PDF (1664KB)

BİLİM HABERLERİ

Olası Yan Etkileri İle Aspartam

Sepril NEBİOĞLU (*)

(*) Ankara Üniversitesi, Eczacılık Fakültesi, Biyokimya Anabilim Dah. Ankara.

Pages, 64-67. | PDF (332KB)

Journal of Pharmaceutical SciencesSunday January 1st, 1989Monday June 18th, 2018

Morphological Investigations on the Diagnostic Features of Six Hypericum Species of the Ukrainian Flora

Valentyna MINARCHENKO* , Oksana FUTORNA** , Vitalii PIDCHENKO***° , Iryna TYMCHENKO**** , Tetyana DVIRNA***** , Larysa MAKHYNIA******

* ORCID: 0000-0002-5049-7620, M.G. Kholodny Institute of Botany, National Academy of Sciences of Ukraine 2 Tereshchenkivska Str., Kyiv 01004, Ukraine;
O.O. Bogomolets National Medical University. 22 Pushkinska Str., Kyiv 01004, Ukraine
** ORCID: 0000-0002-3713-6644, M.G. Kholodny Institute of Botany, National Academy of Sciences of Ukraine 2 Tereshchenkivska Str., Kyiv 01004, Ukraine
*** ORCID: 0000-0003-0850-6666, O.O. Bogomolets National Medical University. 22 Pushkinska Str., Kyiv 01004, Ukraine
**** ORCID: 0000-0001-7505-3164, M.G. Kholodny Institute of Botany, National Academy of Sciences of Ukraine 2 Tereshchenkivska Str., Kyiv 01004, Ukraine
***** ORCID: 0000-0002-9279-9766, M.G. Kholodny Institute of Botany, National Academy of Sciences of Ukraine 2 Tereshchenkivska Str., Kyiv 01004,
Ukraine; O.O. Bogomolets National Medical University. 22 Pushkinska Str., Kyiv 01004, Ukraine
****** ORCID: 0000-0002-8095-4255, O.O. Bogomolets National Medical University. 22 Pushkinska Str., Kyiv 01004, Ukraine

° Corresponding Author: Vitalii Pidchenko
Phone: +380937670224; e-mail: pidchenkovitalii@gmail.com

SUMMARY

The results of comparative analysis of the main diagnostic features of the medicinal raw material of six species of the genus Hypericum of Ukraine are presented. The most important diagnostic features of H. alpigenum Kit, H. elegans Steph. ex Willd., H. hirsutum L., H. maculatum Crantz, H. montanum L., and H. perforatum L. are the localization, form, and color of secretory structures. Characteristics of the basic morphological features of leaves, sepals, petals, and stems of the studied species are provided. It is emphasized that a comprehensive analysis of the species-specific peculiarities of the main raw organs of species of the genus Hypericum allows us to determine their species affiliation clearly. The use of these features makes it impossible to intentionally falsify or incorrectly identify the raw material of a particular species of St. John’s worth during merchandising analysis.

Key Words:

Diagnostic features, Hypericum, medicinal raw materials, leaves, sepals, petals, stems, secretory structures, Ukraine

Enhancing Skin Penetration: The Role of Microneedles

Bülent SAMANCI*º , Fatma Gülgün YENER** , İsmail Tuncer DEĞİM***

* ORCID: 0000-0002-7198-5375, Pharmaceutical Technology Department, Faculty of Pharmacy, Dicle University, Diyarbakir, Turkey,
** ORCID: 0000-0002-7234-0034, Proffesor, Pharmaceutical Technology Department, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey
*** ORCID: 0000-0002-9329-4698, Proffesor, Pharmaceutical Technology Department, Faculty of Pharmacy, Biruni University, Istanbul, Turkey

º Corresponding Author: Bülent SAMANCI
Phone: +904122411000-7531; e-mail: bulent.samanci@dicle.edu.tr

SUMMARY

Since transdermal delivery systems provide some important advantages over oral delivery systems and parenteral delivery systems, they have attracted the attention of researchers. Degradation of the drug in the gastrointestinal (GI) system, irritation of the GI system tract, and the first-pass effect of the drug are some of the disadvantages of oral administration, while the need for medical staff to administer it and creating phobia in the patient are among the disadvantages of parenteral administration. To overcome these drawbacks, researchers have developed formulations for the transdermal delivery of drugs. The most important handicap of transdermal drug administration is the Stratum Corneum layer (St. Corneum), which forms the enormous barrier layer of the skin. Some techniques have been developed to overcome this serious barrier problem of the skin. Microneedles are one of the physical methods to increase the penetration of therapeutic agents through the skin. Microneedles consist of needle arrays long enough to deliver the drug to the dermis layer and micron-sized enough to not reach the nerve cells and not cause pain. Microneedles can
be classified into five different types as solid microneedles, dissolving microneedles, hollow microneedles, coated microneedles, and hydrogel microneedles according to the properties of the materials used in the fabrication and the mechanisms of release of the therapeutic agent. Microneedles can be used in the application of vaccines, proteins, nucleotides, drug delivery systems, cosmetic, and for diagnostic purposes. Although important technological developments have been experienced for microneedle in many areas such as drug delivery systems, disease diagnosis, and cosmetics in the last two decades, there are many working areas that need to be developed. Especially in longterm treatments, studies should be done to develop them as smart devices.

Key Words:

Drug Delivery, Intradermal, Microfabricated device, Microneedle, Skin Penetration, Transdermal.

Bioactivities of A Major Compound from Arthrinium rasikravindrae An Endophytic Fungus of Coleus amboinicus Lour.

Puji ASTUTI°* , Dwi Koko PRATOKO** , Rollando ROLLANDO*** , Giri Wisnu NUGROHO**** , Subagus WAHYUONO***** , Triana HERTIANI****** , Arief NURROCHMAD*******

* ORCID: 0000-0003-3316-6149, Pharmaceutical Biology Department, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia 55281
** ORCID: 0000-0001-7262-4515, Faculty of Pharmacy, Universitas Jember, Jember, Indonesia
*** ORCID: 0000-0001-6210-6247, Program of Pharmacy, Faculty of Science and Technology, Ma Chung University, Malang, Indonesia
**** ORCID: 0000-0001-9086-3181, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia 55281
***** ORCID: 0000-0002-1374-4506, Pharmaceutical Biology Department, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia 55281
****** ORCID: 0000-0002-1756-2478, Pharmaceutical Biology Department, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia 55281
******* ORCID: 0000-0001-7597-2574, Pharmacology and Clinical Pharmacy Department, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia

°Corresponding author: Puji Astuti
Phone/Fax: +62-274-543120; e-mail: puji_astuti@ugm.ac.id

SUMMARY

Many studies reported the ability of endophytic fungi to produce various bioactive compounds having therapeutic values. An endophytic fungus identified as Arthrinium rasikravindrae was isolated from the stem of Coleus amboinicus Lour. This study examined cytotoxic and antimicrobial activities of a major compound isolated from ethyl acetate extract of the fungus fermentation broth. Cytotoxic activities were conducted using MTT assay against T47D, MCF-7, WiDr, 3T3, and Vero cells. IC50 values against Staphylococcus aureus and Escherichia coli were used as the parameters for determining antimicrobial activities. The isolated compound appeared as a single peak in HPLC chromatogram (98.55 %), displayed the highest cytotoxic activity on WiDr cells (IC50 35.03 ± 2.08 μg/mL) and antimicrobial activities against S. aureus (IC50 232.10 ± 1.20 μg/mL) and E. coli (243.59 ± 1.32 μg/mL). Analysis of the UV spectrum and TLC data generated by various detection reagents revealed that the compound was predicted as an N-containing substance having conjugated double bonds.

Key Words:

Coleus amboinicus Lour., cytotoxicity, antimicrobial, Arthrinium rasikravindrae, endophyte, fungus.

Effects of Pycnogenol and Its Combinations with Cisplatin on Hepatocellular Carcinoma Cell Viability

Merve BECİT*,° , Sevtap AYDIN DİLSİZ** , and Nurşen BAŞARAN***

* ORCİD: 0000-0002-8084-4419, Department of Pharmacology, Faculty of Pharmacy, Ataturk University, Erzurum, 25240, TURKEY
** ORCİD: 0000-0002-6368-2745, Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Hacettepe University, Ankara, 06100, TURKEY
*** ORCİD: 0000-0001-8581-8933, Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Hacettepe University, Ankara, 06100, TURKEY

° Corresponding Author: Merve BECİT
Phone: +904422315241; Fax: +904422315201; e-mail: mervebecit@hotmail.com

SUMMARY

Many challenges of hepatocellular carcinoma treatment, such as side effects and drug resistance, still remain. Therefore, new improvements with high pharmaceutical function and low toxicity
are needed. Recently, the efficacy of the combination therapy of antineoplastic drugs with natural products like pycnogenol has garnered attention. Pycnogenol® is a standardized extract from the bark of Pinus pinaster and consists of phenolic compounds. Pycnogenol is considered complementary in the treatments of some cancer besides its good tolerability and high safety. This study aims to reveal the synergistic effects of pycnogenol combination with cisplatin and its relation to human hepatocellular carcinoma (HepG2) cell viability. Effects of single and combined treatment on cell viability were evaluated in Chinese hamster lung fibroblasts (V79) and HepG2 cells using MTT assay. In HepG2 cells, this combined treatment showed a more cytotoxic effect than singledose
groups. Pycnogenol increased the cytotoxicity of cisplatin at 500 μM for 24 h; at 250-500 μM for 48 h in V79 cells; and also, at 125-500 μM for 24 h; at 62.5-500 μM for 48 h in HepG2 cells (p<0.05). Our study is the first study to show that pycnogenol treatment with cisplatin has been combined in the HepG2 cell line. As a result, pycnogenol induced cisplatin cytotoxicity via combined treatment on HepG2 cells and exhibited a synergistic effect with cisplatin. In conclusion, pycnogenol may play a role in the chemotherapy of hepatocellular carcinoma; however, further
studies are required to confirm their interactions with cisplatin.

Key Words:

Pycnogenol, cisplatin, MTT, cancer, hepatocellular carcinoma, HepG2 cells.

Improvement in Aqueous Solubility of Cilnidipine by Amorphous Solid Dispersion, Its Formulation into Interpenetrating Polymer Network Microparticles and Optimization by Box-Behnken Design

Amit KUHIKAR* , Shagufta KHAN**° , Komal KHARABE*** ,
Dilesh SINGHAVI**** , Girish DAHIKAR*****

* ORCID: 0000-0001-7353-9814, Institute of Pharmaceutical Education and Research, Borgaon (Meghe) Wardha, Maharashtra, India.
** ORCID:0000-0002-2827-7939, Institute of Pharmaceutical Education and Research, Borgaon (Meghe) Wardha, Maharashtra, India.
*** ORCID: 0000-0002-5237-6929, Institute of Pharmaceutical Education and Research, Borgaon (Meghe) Wardha, Maharashtra, India.
**** ORCID: 0000-0002-2544-7226, Institute of Pharmaceutical Education and Research, Borgaon (Meghe) Wardha, Maharashtra, India.
***** ORCID: 0000-0002-2284-535X, Institute of Pharmaceutical Education and Research, Borgaon (Meghe) Wardha, Maharashtra, India.

°Corresponding Author: Shagufta Khan, Professor,
Phone: (+91)7152-240284, Fax (+91)7152-241684; e-mail: shaguftakhan17@rediffmail.com

SUMMARY

Cilnidipine(CPN), a Biopharmaceutics Classification System class II drug, has dissolution rate-limited bioavailability and a very short half-life (20.4 min). Thus, there is a need to improve the solubility and prolong the drug release so that the therapeutic concentration of CPN could be maintained for a prolonged time. Therefore, the present investigation was aimed to improve the solubility of CPN by preparing amorphous solid dispersion (ASD) and sustain its release by incorporating CPN loaded ASD (CPNASD) in interpenetrating polymer network (IPN) microparticles. ASD was prepared using Solutol HS 15 and Gelucire®50/13. Solutol HS 15 provided a better effect by increasing 84.09 folds solubility of CPNASD in water as compared to the free CPN, therefore it was used in the formulation of IPN microparticles. Characterization of ASD by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) confirmed a decrease in the crystallinity
of CPN. IPN microparticles loaded with CPNASD were prepared by varying chitosan concentrations, polyvinyl alcohol (PVA), and massratio of chitosan:TPP and optimized by Box-Behnken Design. The constraints on the responses were maximum drug entrapment efficiency and sustained drug release with more than 80% drug release in 12 h. IPN microparticles with composition, chitosan 50mg, PVA 74.99mg (Volume of aqueous phase; 10 ml, Volume of organic phase; 50 ml) and chitosan:TPP 2.52 was the predicted optimized condition by the software and IPN with this composition provided high % entrapment efficiency (83.87±0.85) and sustained release (83.29±0.55) for 12 h. Solutol HS 15 was successful in providing a massive increase in solubility of CPN, and a uniform sustained release was achieved by loading CPNASD in IPN microparticles.

Key Words:

Cilnidipine, Solid dispersion, Solutol HS 15, Interpenetrating polymer network microparticles, Chitosan, Polyvinyl alcohol.