Volume 11

October-December 2019

Research Articles

Olubunmi Olayemi, Mercy Aboh, Christianah Isimi

Herbal medicine has been used in the treatment of many diseases including those superficial infections on the skin. Alchornea cordifolia is widely distributed in the tropical region of Africa and is used traditionally as a remedy for healing wounds and skin infections. This study was carried out to prepare acceptable topical semisolid formulations containing the hydro-alcohol leaf extract of Alchornea cordifolia. The dried leaves of Alchornea cordifolia was macerated in 50 % v/v hydro-ethanol for 72 h, the resulting dried extract (ACLE) was incorporated at concentrations of 5 and 10 %w/w into an ointment and a cream base to prepare ACLE ointments and ACLE oil in water creams. Organoleptic and physiochemical properties of the ACLE formulations were evaluated using standard procedures. Invitro antimicrobial activity of the prepared ointments and creams against selected microorganisms was also carried out using the agar dilution method. All the ointment and cream formulations exhibited good physicochemical properties, in addition, they were found to be physically stable after storage at room temperature for 30 days. Cream formulations containing 5 % ACLE showed strong inhibition against bacteria and fungi organisms.

Keywords: Alchornea Cordifolia, Ointments, Creams, Physiochemical Properties, In Vitro Antimicrobial Activity.

Sujatha P Muchalambe, A Geethalakshmi, Amar Kumar Gupta

Transdermal therapeutic systems have been designed to provide controlled continuous delivery of drugs via the skin to the systemic circulation. Advantages of transdermal delivery include convenience, comfort, by-pass the first phase hepatic metabolism, and control over drug absorption. Atorvastatin undergoes high intestinal clearance and first-pass metabolism, which is the main cause for the low systemic availability (30%). Food has been shown to reduce the rate and extent of atorvastatin absorption. Administration of atorvastatin with food produces a 25% reduction in Cmax (rate of absorption) and a 9% reduction in AUC (extent of absorption). In present work was designed to develop suitable transdermal matrix type of Atorvastatin calcium, using Hydroxypropyl methylcellulose (HPMC), Eudragit RS 100 and ethyl cellulose (EC) with PEG 400 (as plasticizer) and propylene glycol (as penetration enhancer). The solvent casting technique was employed for the preparation of Atorvastatin calcium transdermal patches. The dry films were evaluated for weight variation, thickness uniformity, moisture content, moisture uptake, folding endurance and % drug content. In-vitro release studies were performed using Franz’s diffusion cell and permeation studies were carried out by using rat skin. The concentration of diffused drug was measured using UV- visible spectrophotometer at λ max 246.2 nm. FT-IR studies revealed that the drug and polymer were compatible with each other and all the batches prepared and evaluated, F1, F4 and F5 showed promising results. It was concluded that HPMC and ethyl cellulose are useful in formulating sustained release Atorvastatin transdermal patches.

Keywords: Transdermal Drug Delivery, Atorvastatin Calcium, HPMC, EC, Eudragit, PEG 400.

Mahajan Harshal D, Wagh Rajendra D, Baviskar Dheeraj T

Ocular bioavailability of drugs from conventional eye drops is very poor due to the physiologic barriers of the eye. In general, ocular efficacy is closely related to ocular drug bioavailability, which may be enhanced by increasing corneal drug penetration and prolonging precorneal drug residence time. Therefore, the present study involves the development, characterization and evaluation of biodegradable moxifloxacin hydrochloride nanoparticles intended for ocular use. Nanoparticles were prepared by nanoprecipitation techniques using Poly D, L-lactide. To optimize the drug formulation, 32 factorial designs was applied. The effect of independent variables such as drug-to-polymer ratio and speed of homogenizers on entrapment efficiency (EE %) and particle size were investigated. Further studies such as differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy were carried out on the optimized formula. In vitro release study showed extended drug release. DSC and XRD indicated the dispersion of the drug within the nanoparticles. Ocular tolerance was evaluated using hen’s egg chorioallantoic membrane (HET-CAM) test which showed nonirritant efficacy of developed formulation. These results demonstrate the feasibility of encapsulating moxifloxacin hydrochloride biodegradable polymeric nanoparticles for ocular delivery.

Keywords: Moxifloxacin Hydrochloride, Poly D, L-lactide, Nanoparticle, Ocular Drug Delivery.

Sunil M Bhadane, Dipak D Patil, Vivekanand K Chatap, Sandip P Patil, Laxmikant R Zawar

The aim of the present study was to enhance the solubility, dissolution rate and thus oral bioavailability of a poorly soluble, BCS class II drug Ziprasidone hydrochloride (ZPH), using its solid dispersions (SDs) with poloxamer 188 (PX) and HPMC E15.Solid dispersions were prepared by co-grinding, kneading, freeze drying and microwave methods. The dispersions were evaluated for various in vitro parameters such as solubility study, dissolution study, fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), scanning electron microscopy (SEM). Microwave generated solid dispersions in 1:5 ZPH – PX ratio exhibited significant improvement in solubility and dissolution rate compared to that of pure drug. The superior dissolution profile observed for microwave induced solid dispersions is attributed to amorphization of the drug by microwaves, improved surfactant and wetting characteristics of the carrier with the drug. Thus, microwave technology offers a simple, efficient, solvent free promising alternative method to prepare solid dispersion of ZPH with significant enhancement of the in vitro dissolution rate.

Keywords: Solid Dispersion, Microwave Method, Freeze Drying Method, Ziprasidone HCL, Poloxamer 188, HPMC E15, Solubility, Dissolution.

Soraya Madoui, Kamel Mokhnache, Hanane Khither, Seoussen Kada, Noureddine Charef

The extract of leaves-flowers mixture of Cytisus triflorus L was selected for their anti-ulcer effect and oral acute toxicity investigation. The acute toxicity method described in European guideline 425, is a method of administering a specified oral dose of 2 g/kg of the extract, to exclude possible toxicity due to extract, a histological study of the liver and kidneys was performed. The results showed the absence of liver and renal toxicity following the administration of the 2 g / kg dose of the crude leaves and flower mixture extract of Cytisus triflorus L. Concerning gastric antiulcer activity, it is necessary to check the protective action of the crude extract at doses 200 mg/kg and 400 mg/kg, against the ulcer caused in animals by administration of an ulcerogenic agent such as ethanol. The evaluation of the gastroprotective effect of the extract was carried out by macroscopic and microscopic analysis which will look at the observable external and internal lesions, as well as an estimate of the percentage of ulceration. The results show a very significant reduction in the areas injured in the Ranitidine treated groups and the crude extract at doses of 200 or 400 mg / kg, with percentages of 0.75 ± 0.16%, 2.71 ± 0.13. % and 1.49 ± 0.14% respectively. The gastroprotective effect of the crude extract at 400 mg/kg is confirmed by the restoration of the normal architecture of the rats’ stomachs. These results confirm the validity of the use of this plant in traditional medicine and offer hope for the development of effective anti-ulcer therapy without side effects.

Keywords: Cytisus Triflorus, Mixture, Anti-Ulcer, Acute Toxicity.


Salima Bacha, Hadj Benhebal, Mohamed Hamdi, Moussa Ahmed, Baghdad Khiati

Numerous previous studies have demonstrated improved wound healing associated with natural-based formulations. Therefore, in the present work, a hydrogel composed of biopolymer gelatin incorporated with bee pollen was chosen to develop BPHG of healing in second degree burn wounds in adult rabbits. A total of 09rabbits with superficial and partial thickness burns were divided into three equal groups randomly by consecutive sampling method, one group were dressed with BPG while the other was treated with paraffin-impregnated tulle gras (PTG). Adult rabbits were anesthetized and dorsum shaved. Cylindrical stainless-steel rod (2×4 cm diameter) was heated to 100℃. Additionally the bee pollen powder used has been characterized by FTIR spectroscopy. On Day 25, Only in the BPHG-treated groups, was degree of wound healing increased up to normal condition. Besides, the healing area of the BPHG-treated wound was better than that of the untreated and PTG- treated groups during 2, 14 and 14 days after burn. In this first approach with BPGH our results provide the first demonstration that bee pollen gel can be considered as a possible alternative for the treatment of burns.

Keywords: Bee Pollen, Na CMC, Burn.

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