The Pharmacological Basis of Therapeutics A Textbook of Pharmacology, Toxicology and Therapeutics for Physicians and Medical Students. By Prof. Louis Goodman and Prof. Alfred Gilman. Pp. xiii + 1383. (New York: The Macmillan Company, 1941.) 50s. net.

The Pharmacological Basis of Therapeutics

Quercetin is a bioactive compound that is widely used in botanical medicine and traditional Chinese medicine due to its potent antioxidant activity. In recent years, antioxidant activities of quercetin have been studied extensively, including its effects on glutathione (GSH), enzymatic activity, signal transduction pathways, and reactive oxygen species (ROS) caused by environmental and toxicological factors. Chemical studies on quercetin have mainly focused on the antioxidant activity of its metal ion complexes and complex ions. In this review, we highlight the recent advances in the antioxidant activities, chemical research, and medicinal application of quercetin.

Antioxidant Activities of Quercetin and Its Complexes for Medicinal Application.

Background Rutin is a common dietary flavonoid which has received great attention in literature, due to their pharmacological properties, including antimicrobial, anti-inflammatory, anticancer, antidiabetic, inter alia . Over 860 products containing rutin are currently marketed in the US. The major disadvantage associated with rutin is its constrained bioavailability, mainly caused by its low aqueous solubility, poor stability and limited membrane permeability. Scope and approach The aim of this contribution is to give an overview of the current methods (conventional and innovative) for the extraction, identification and purification of rutin. Furthermore, recent findings regarding its pharmacological activities and the different approaches to increase rutin solubility in both aqueous and lipid phases will be discussed. Key findings and conclusions Current trends on extraction process have been focused on the discovery and design of green and sustainable extraction techniques to optimize the recovery of rutin. Despite the bioactivity expressed in different in vitro systems, its biological effects in vivo are limited by the poor bioavailability of the flavonoid. The utilization of delivery systems for rutin or its enzymatic or chemical transformation towards highly soluble derivatives have the potential to improve rutin bioavailability, as well as its stability and/or specific biological properties. These novel rutin formulations may bring this promising flavonoid to the forefront of nutraceuticals for the prevention and/or treatment of various chronic human diseases.

Rutin: A review on extraction, identification and purification methods, biological activities and approaches to enhance its bioavailability

Introduction: Natural compounds such as bioflavonoids have found application in health care system due to their wide biological activities, high safety margins and lower cost. Rutin, a polyphenolic bioflavonoid has shown wide range of pharmacological applications due to its significant antioxidant properties. Conventionally, it is used as antimicrobial, antifungal, and antiallergic agent. However, current research has shown its multispectrum pharmacological benefits for the treatment of various chronic diseases such as cancer, diabetes, hypertension and hypercholesterolemia. Its use is advantageous over other flavonoids as it is a nontoxic and nonoxidizable molecule. Areas covered: This review focus on various studies done on rutin explaining its broad spectrum pharmacological activities. In addition, this review will also focus on the challenges associated with the drug and various approaches to improve the oral bioavailability of rutin. Expert opinion: Rutin is a highly potent molecule due to its strong...

Rutin : therapeutic potential and recent advances in drug delivery.

Platelet-rich plasma (PRP) has emerged as a new treatment modality in regenerative plastic surgery, and preliminary evidence suggests that it might have a beneficial role in hair regrowth. Here, we report the results of a randomized, evaluator-blinded, placebo-controlled, half-head group study to compare, with the aid of computerized trichograms, hair regrowth with PRP versus placebo. The safety and clinical efficacy of autologous PRP injections for pattern hair loss were investigated. PRP, prepared from a small volume of blood, was injected on half of the selected patients’ scalps with pattern hair loss. The other half was treated with placebo. Three treatments were administered to each patient at 30-day intervals. The endpoints were hair regrowth, hair dystrophy as measured by dermoscopy, burning or itching sensation, and cell proliferation as measured by Ki67 evaluation. Patients were followed for 2 years. Of the 23 patients enrolled, 3 were excluded. At the end of the 3 treatment cycles, the patients presented clinical improvement in the mean number of hairs, with a mean increase of 33.6 hairs in the target area, and a mean increase in total hair density of 45.9 hairs per cm2 compared with baseline values. No side effects were noted during treatment. Microscopic evaluation showed the increase of epidermis thickness and of the number of hair follicles 2 weeks after the last PRP treatment compared with baseline value (p < .05). We also observed an increase of Ki67+ keratinocytes in the epidermis and of hair follicular bulge cells, and a slight increase of small blood vessels around hair follicles in the treated skin compared with baseline (p < .05). Relapse of androgenic alopecia was not evaluated in all patients until 12 months after the last treatment. After 12 months, 4 patients reported progressive hair loss; this was more evident 16 months after the last treatment. Those four patients were re-treated. Our data clearly highlight the positive effects of PRP injections on male pattern hair loss and absence of major side effects. PRP may serve as a safe and effective treatment option against hair loss; more extensive controlled studies are needed.

https://stemcellsjournals.onlinelibrary.wiley.com/doi/pdf/10.5966/sctm.2015-0107

The Effect of Platelet-Rich Plasma in Hair Regrowth: A Randomized Placebo-Controlled Trial

Hair has psychological and sociological importance throughout the ages in framing the personality and general appearance of an individual. Significant progress is being made on discovering an effective and safe drug for hair growth. Angiogenesis, androgen antagonism, vasodilation, potassium channel opening and 5-alpha reductase inhibition are the major non-surgical therapeutic strategies of hair growth promotion. In spite of a flood of drugs claiming to be useful as hair growth promoters, more rational strategies, which can target the problem areas or stages of the hair growth cycle effectively, are still awaited. This article highlights the developments in hair rejuvenation strategies and reviews the potential of herbal drugs as safer and effective alternatives.

Hair growth and rejuvenation: An overview

Development of amphiphilic drug-lipid complexes is a potential approach for improving therapeutic efficacy of the drugs by increasing solubility, release profile and oral bioavailability. Quercetin (3, 3, 4, 5, 7-pentahydroxyflavone), a polyphenolic flavonoid, shows several biological effects like anti-inflammatory, anti-cancer, antiproliferative, antimutagenic and apoptosis induction but its use is limited due to its low aqueous solubility. To overcome this limitation, a value added phospholipid complex of quercetin was developed to improve its aqueous solubility for better absorption through the gastrointestinal tract and this might result in improved bioavailability. The quercetin-phospholipid complex thus prepared was evaluated for various physico-chemical parameters like infra red spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), scanning electron microscopy (SEM) and solubility study. The In vitro antioxidant activity was also studied. The phospholipid complex of quercetin was found to be fluffy and porous with rough surface in SEM. FTIR, DSC and XRPD data confirmed the formation of phospholipid complex. The water solubility of quercetin was improved by 12 folds (from 3.44 μg/ ml to 36.81 μg/ ml) in the prepared complex. There was no statistical difference between the quercetin complex and quercetin in the In vitro anti-oxidant activity, indicating that the process of complexation did not adversely affect the bioactivity of the active ingredient.

Quercetin-phospholipid complex: an amorphous pharmaceutical system in herbal drug delivery.

Biopharmaceutical properties together with potency contribute critically towards clinical efficacy of the drugs by influencing the dissolution and bioavailability. The aim of this study was to develop an amphiphilic phyto-phospholipid complex in order to enhance the delivery of poorly soluble rutin. The rutin-phospholipid complex (Ru-PLc) was prepared and investigated for various physico-chemical parameters like drug loading, infrared absorption (FTIR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), scanning electron microscopy (SEM), aqueous/ n-octanol solubility and dissolution study. The in vitro anti-oxidant activity was also studied. In the SEM, Ru-PLc was found fluffy and porous with rough surface morphology. FTIR, DSC and XRPD data confirmed the formation of phospholipid complex. The water/ noctanol solubility of rutin was improved from 2.88 to 45.71 μg/ ml and 68.17 to 245.18 μg/ ml, respectively in the complex. The improved dissolution was shown by the phospholipid complex at different pH buffers. The antioxidant activity indicated that, the bioactivity of rutin was maintained even after being complexed with the phospholipid. Based on the results, it can be concluded that the phospholipid complex may be considered as a promising drug delivery system for improving the overall absorption and bioavailability of the rutin molecule.

Rutin-phospholipid complex: an innovative technique in novel drug delivery system- NDDS.

For improving bioavailability in controlled release fashion and to circumvent the hepatic first pass effect of glipizide mucoadhesive buccal films of glipizide were prepared by solvent casting technique. Buccal films were prepared using hydroxy propylmethylcellulose, sodium carboxymethylcellulose, carbopol- 934P and Eudragit RL-100. Films were evaluated for their weight, thickness, surface pH, swelling index, in vitro residence time, folding endurance, in vitro release, ex vivo permeation studies and drug content uniformity. The films exhibited controlled release over more than 6 h. From the study it was concluded that the films containing 5 mg glipizide in 4.9 % w/v hydroxy propylmethylcellulose and 1.5 % w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release thus proved to be potential candidate for the development of buccal films for therapeutic use.

http://www.ijpsnonline.com/Issues/184.pdf

Mona Semalty

Papers

Hair growth and rejuvenation: An overview

Quercetin-phospholipid complex: an amorphous pharmaceutical system in herbal drug delivery.

Rutin-phospholipid complex: an innovative technique in novel drug delivery system- NDDS.

Development of Mucoadhesive Buccal Films of Glipizide

Gallic Acid-Phospholipid Complex: Drug Incorporation and Physicochemical Characterization