Gamal M. El Maghraby

Tanta University · Faculty of Pharmacy

The aim was to investigate eutectic transition during tableting and storage. Mixtures of lidocaine and series of NSAIDs with increasing melting point were used as model systems to guide formulators to scaleup eutectic forming materials gaining enhanced dissolution while avoiding deleterious physical changes. Physical mixtures of NSAIDs with lidocai...

The aim of this work was to improve dissolution rate and antibacterial activity of cefpodoxime proxetil (CP) by Pluronic PE 6800 (Poloxamer 188) as eutectic forming hydrophilic polymer. CP was incorporated in the polymer by melt granulation technique. CP was mixed with melted polymer before addition of Avicel, in absence and presence of HPMC E6, wi...

Lamotrigine is an antiepileptic drug with slow dissolution rate which can reduce its oral bioavailability. In addition, it was reported to have first pass metabolism. Accordingly, the aim of this work was to enhance its dissolution rate utilizing co-crystallization technique to be suitable for incorporation in buccal dosage form. L-proline was sele...

In the recent decades, prostaglandins were recommended as a new therapeutic modality of stable vitiligo with promising efficacy. Therefore, we designed the current work to compare the significance of two different subtypes of prostaglandins [prostaglandin E2 (PGE2) versus prostaglandin F2 alpha (PGF2α)], assisted with NB-UVB phototherapy, in treatm...

Introduction: Tranexamic acid (TXA) is a promising treatment modality for melasma. Microneedling (MN) and fractional carbon dioxide (CO2) laser were reported to enhance TXA transepidermal delivery. Objectives: To compare efficacy and safety of topical TXA alone or in combination with either fractional CO2 laser or MN for treatment of melasma. M...

Introduction: Hyperhidrosis is excessive sweating beyond thermoregulatory needs. It is a potentially disabling condition with challenging management. Aluminum chloride is the established topical treatment; however, response remains unsatisfactory. Oxybutynin is an anticholinergic drug that stands as a therapeutic chance for hyperhidrosis. Objecti...

The aim was to enhance the dissolution rate and in vivo efficacy of flubendazole against trichinella spiralis. Flubendazole nanocrystals were developed by controlled anti-solvent recrystallization. Saturated flubendazole solution was prepared in DMSO. This was injected into phosphate buffer (pH 7.4) containing Aerosil 200, Poloxamer 407 or sodium l...

The goal was to scrutinize niosomes as potential carriers for enhanced efficacy of norfloxacin against Toxoplasma gondii RH strain. This was assessed in vitro and in vivo. Standard niosomes of Span 60 and cholesterol were prepared. Gelucire 48/16 or Tween 80 was incorporated as hydrophilic fluidizer. The prepared vesicles were characterized for sha...

The ubiquitous emergence of bacterial resistance is a challenging problem in infectious diseases treatment. Recently, new research lines employed nano-drug delivery systems to enhance antibacterial activity of the existing antibiotics. Accordingly, the objective of this study is to optimize surfactant nanovesicles to improve the antimicrobial effec...

Aim: The aim of this study was to investigate the potential cardioprotective and anti-cancer effects of carvedilol (CAR) either free or as loaded nano-formulated with or without doxorubicin (DOX) in solid Ehrlich carcinoma (SEC)-bearing mice. It focused on assessment of cardiac damage, drug resistance, apoptosis, oxidative stress status, angiogene...

Unlabelled: Latent toxoplasmosis mostly reactivates which could result in acute encephalitis. Chronic toxoplasmosis treatments are severely constrained by Toxoplasma cyst resistance. Novel therapeutic approaches are therefore becoming more essential. In this study, the effects of levamisole (LEVA) and spiramycin on the early and late stages of exp...

Objectives: The aim of this work was to investigate the regional difference in linagliptin intestinal membrane transport and to investigate the effects of carvedilol, atorvastatin and bile salts on intestinal absorption of linagliptin. Methods: The study employed an in-situ rabbit intestinal absorption technique. The membrane transport parameter...

omega 3 new formulations as pulpotomy agents

Background: Eslicarbazepine acetate (ESL) is antiepileptic agent which is approved for use as single therapy or in combination with other drugs. However, it suffers from poor oral bioavailability. Modulation of drug crystallinity can be utilized as an approach for enhancing drug dissolution. Objective: Accordingly, the aim of this study was to i...

Toxoplasmosis is a disease with a worldwide distribution and significant morbidity and mortality. In search of effective treatment, mefloquine (MQ) was repurposed and loaded with niosomes to treat acute and chronic phases of toxoplasmosis in experimental mice. Mice were orally inoculated with 20 cysts of Toxoplasma gondii (ME 49 strain) for the acu...

The aim of this study was to develop microemulsion (ME) formulation with possible phase transition into liquid crystals upon ocular application to enhance acetazolamide bioavailability. Pseudoternary phase diagrams were constructed using olive oil or castor oil (oily phase), Tween 80 (surfactant), and sodium carbonate solution (aqueous phase). Micr...

The clinical utility of doxorubicin is compromised due to dose related toxic side effects and limited oral bioavailability with no oral formulation being marketed. Enhancement of intestinal absorption and magnification of cytotoxicity can overcome these limitations. Accordingly, the objective was to probe penetration enhancers, bilosomes and their...

Lopinavir is effective in treatment of HIV infection but experiences low oral bioavailability due to poor solubility, pre-systemic metabolism, and P-gp intestinal efflux. Co-processing with menthol enhanced its dissolution and intestinal permeability. Niosomes comprising Span 60, cholesterol and poloxamer 407 were formulated in absence and presence...

Background: Many therapeutic modalities were reported for the treatment of warts; however, no single treatment is completely effective. Objective: To evaluate the efficacy of intralesional injection of MMR vaccine vs vitamin D in treatment of warts. Patients and Methods: A total of 60 patients were included in the study divided into two groups. Gro...

Lopinavir is an antiretroviral, antiparasitic agent and recently utilized in treatment of COVID-19. Unfortunately, lopinavir exhibited poor oral bioavailability due to poor dissolution, extensive pre-systemic metabolism, and significant P-glycoprotein intestinal efflux. Accordingly, the aim was to enhance dissolution rate and intestinal absorption...

Background: Instant disintegration of oral disintegrating tablets (ODTs) provides greater chance for buccal absorption, avoiding presystemic metabolism of nimodipine. In addition, ODT can be easily dispersed in suitable liquid before delivery via nasogastric tube in critical care setting. Objective: The objective was to improve nimodipine dissoluti...

The study investigated Eudragit coated microemulsion (ME) for oral delivery of spiramycin in treatment of toxoplasmic encephalitis. The goal was to augment the efficacy of ME by protection from gastrointestinal conditions and/or providing bioadhesion. Uncoated and coated MEs comprise labrafil as oil, cremophore EL as surfactant and labrasol as cosu...

Purpose: The aim of this work was to probe cubosomes for enhanced intestinal absorption and oral bioavailability of poorly absorbable fexofenadine HCl (FEX-HCl). Materials and methods: Two cubosomal systems were fabricated utilizing glyceryl mono-oleate, a lyotropic mono lamellar lipid as oil phase and poloxamer407 as stabilizer at weight ratios...

Burn wound infections with multidrug-resistant (MDR) bacteria are shown in many countries as severe widespread health threats. Consequently, attention has been devoted to new nanoparticle-based materials in the field of antimicrobial chemotherapy for burn wound infections. This study aimed to evaluate both in vitro and in vivo efficacies of nanopar...

Atorvastatin is the most commonly used hypolipidemic drug. It provides excellent protection against cardiovascular disease especially in subjects having high risk factors. However, atorvastatin has problematic biopharmaceutical characteristics due to low dissolution rate and extensive pre-systemic disposition. This contributed to reduced oral bioav...

Self-microemulsifying systems undergo self-dispersion to form microemulsion with subsequent self-assembly to form liquid crystalline (LC) and/or gel phases. These transitions modulate the release and absorption pattern of loaded drug. Accordingly, the primary objective was to evaluate these phases with respect to gliclazide release and absorption a...

The oral absorption and hence the oral bioavailability of carbamazepine (CBZ) is variable even after administration of rapidly dissolving formulation. This problem was attributed to supersaturation of CBZ and transformation to the less soluble carbamazepine dihydrate (CBD). Accordingly, formulation of sustained release products of CBZ is a promisin...

Ivermectin (IVM) is one of the competitive treatments used for trichinellosis. However, several studies linked its efficacy with early diagnosis and administration to tackle the intestinal phase with limited activity being recorded against encysted larvae. The aim of this study was to employ niosomes for enhancing effectiveness of oral IVM against...

Apigenin is a natural flavonoid which is claimed to have many pharmacological activities ranging from simple anti-inflammatory to anticancer action. However, poor dissolution slowed the advancement of this drug through the development pipelines. The objective of this work was to probe ethanol aided kneading of apigenin with arginine as a new strate...

WHO considers praziquantel (PZQ) as the drug of choice for treatment of Schistosoma mansoni infection but this requires high dose due to poor solubility and first pass metabolism. The aim of this work was to optimize nanostructured lipid carriers (NLCs) for enhanced PZQ oral delivery. The optimization involved testing the effect of surface charge o...

The oral absorption and hence the oral bioavailability of carbamazepine (CBZ) is variable even after administration of rapidly dissolving formulation. This problem was attributed to supersaturation of CBZ and transformation to the less soluble carbamazepine dihydrate (CBD). Accordingly, formulation of sustained release products of CBZ is a promisin...

Co-application of local anesthetics as lidocaine and nonsteroidal anti-inflammatory drugs (NSAIDs) can enhance local analgesia. Co-formulation of lidocaine with NSAIDs can modulate physicochemical properties like melting point which can affect transdermal delivery. The purpose was to probe lidocaine as eutectic forming drug for enhanced transdermal...

Development of fixed dose combinations is growing and many of these drug combinations are being legally marketed. However, the development of these requires careful investigation of possible physicochemical changes during co-processing. This requires investigation of the effect of co-processing of drug combination in absence of excipients to maximi...

Cefdinir is an orally active antimicrobial agent used in treatment of various respiratory tract infections. It is a class IV drug having low dissolution rate which resulted in poor oral bioavailability. Nanographene oxide was utilized as a drug carrier to enhance the dissolution rate and antibacterial activity of cefdinir. Synthesis of graphene oxi...

Background: Cilostazol is an anti-platelets drug with considerable antithrombotic effects in vivo. Therefore, it is widely used by elderly patients. However, it suffers from poor bioavailability due to its low aqueous solubility. The objective of this work was to enhance the dissolution of cilostazol with the aim of formulating fast dissolving tabl...

Sustaining and controlling the rate of drug release is essential in pharmaceutical technology. It can reduce the number of units administered by the patient with subsequent improvement in patient compliance. These technologies can allow controlled liberation of the active pharmaceutical ingredients to correlate with the chronobiology of the disease...

INTRODUCTION The dissolution of many drugs is the determining rate step for bioavailability and absorption after the drug oral administration. More than 40% of developed drugs and more than 70% of synthesized drugs suffer from poor dissolution rate and bioavailability. These new chemical interties are commonly classified under the Class II categori...

Objective: The aim of this work was to investigate dry co-grinding of nateglinide with meglumine for enhanced dissolution rate of nateglinide. The study was extended to investigate the effect of this dissolution enhancement on the hypoglycemic effect of the drug in diabetic rats. Methods: Nateglinide was subjected to dry co-grinding with increas...

ABSTRACT Olmesartan Medoxomil (OM) is an angiotensin-receptor blocker. Based on the solubility and permeability, (OM) is classified as class II drug according to the biopharmaceutics classification system (BSC), meaning that the drug is poor soluble. This is believed to be responsible for its low bioavailability. Therefore, the objective of this st...

The short residence time, corneal barrier functions, and other effective eye protective mechanisms limited the ocular availability after topical application. Ocular inserts are being developed as polymer films for insertion into the conjunctival sac with the goal of increasing ocular availability. Unfortunately, these devices are not convenient for...

Cancers are life threatening diseases and their traditional treatment strategies have numerous limitations which include poor pharmacokinetic profiles, non-specific drug distribution in the body tissues and organs and deprived tumor cells penetration. This attracted the attention of researchers to tailor efficient drug delivery system for anticance...

Meloxicam is a widely used non-steroidal anti-inflammatory agent. However, its erratic and poor dissolution delays its onset of action. Dissolution enhancement of such medicine is essential to obtain rapid pain relief. Amino acids showed high potential to enhanced dissolution rate of drugs after co-processing. Accordingly, the objective of this wor...

The study investigated chitosan coated nanostructured lipid carriers (NLCs) for oral delivery of albendazole in treatment of trichinellosis. NLCs comprised precirol and oleic acid with Tween and Span 80. Dicetylphosphate was used as charging agent to allow chitosan coating. Trichinella spiralis infected mice were used and albendazole suspension, co...

Background: Many therapeutic modalities were reported for the treatment of warts; however, no single treatment is completely effective. Objective: To evaluate the efficacy of intralesional injection of MMR vaccine vs vitamin D in treatment of warts. Patients and methods: A total of 60 patients were included in the study divided into two groups...

Background Melasma is a common cause of cosmetic disfigurement in the face. This facial hyperpigmentation leads to many psychological problems. It is difficult to be treated and has a high rate of recurrence. Objective The aim of this study was to evaluate and compare the efficacy of topical tranexamic acid 5% versus topical flutamide 1% in the tre...

Fenofibrate is antihyperlipidemic which has low and variable oral bioavailability due to erratic dissolution characteristics. Niacin showed a potential atheroprotective effects suggesting possible co-administration with fenofibrate with a potential for development of fixed dose combination. The chemical structure of both drugs highlights the opport...

Background: Nimodipine is calcium channel blocker frequently used in critical care settings. It is mainly absorbed from upper gastrointestinal tract. Accordingly, development of gastroretentive formulation will be beneficial. The benefit would be maximized for critical care patients if the developed system was in liquid form to facilitate administr...

Acyclovir (ACV) is widely used in the treatment of herpes encephalitis. The present study was conducted to prepare chitosan-tween 80 coated solid lipid nanoparticles (SLNs) as a delivery system for brain targeting of ACV in rabbits. The SLNs were prepared and coated in one step by microemulsion method using a coating solution containing chitosan (0...

The goal of this study was to design, optimize, and characterize Acyclovir - loaded solid lipid nanoparticles (ACV-SLNs) concerning particle size, zeta potential, entrapment efficiency, and release profile. Full factorial design (2³) was applied and the independent variables were surfactant type (Tween 80 and Pluronic F68), lipid type (Stearic acid...

Objectives: Development and evaluation of rapidly dissolving film for intra-oral administration of naftopidil. Significance: Formulation of naftopidil in the form of rapidly dissolving buccal film can eliminate the dissolution problem of naftopidil and provide greater chance for direct absorption into the systemic circulation bypassing the presyste...

Background: Schistosomiasis is one of the most prevalent parasitism and remains a major cause of morbidity in the world. Hepatic fibrosis is considered the major morbid sequel of schistosomiasis. Praziquantel (PZQ) is the only recommended drug by the WHO against all Schistosoma spp. However, it exhibits low and erratic bioavailability and drug resi...

Nebivolol hydrochloride is an antihypertensive agent which is classified as class II drug. Its oral bioavailability is variable due to its poor dissolution and pre-systemic metabolism. The aim of this work was to enhance the dissolution rate of nebivolol hydrochloride both in saliva pH (pH 6.8) and in gastric conditions (pH 1.2). This was done with...

Fast dissolution of nonsteroidal anti-inflammatory drugs (NSAIDs) is a prerequisite from patient perspective. However, most NSAIDs are slowly dissolving acidic compounds. Caffeine, a commonly used analgesic adjuvant with NSAIDs showed high potential as eutectic co-former for acidic compounds. The study investigated eutectic forming potential of caf...

Flutamide is an orally active anti-androgenic agent of non-steroidal origin which is approved for treatment of prostatic carcinoma. It has low and variable oral bioavailability. This is mainly attributed to its poor dissolution behavior. Co-crystallization of drugs with inert co-former is an emerging technique for enhancing dissolution rate. Accord...

Objectives: Enhance the dissolution rate of bicalutamide via co-crystallization with sucralose (sweetener), with the aim to develop rapidly disintegrating tablets with subsequent prompt dissolution. Significance: Bicalutamide is antiandrogenic agent for the treatment of prostate cancer but has low and variable oral bioavailability, mainly attribute...

Praziquantel (PZQ) is recommended by the WHO as the first line in treatment of schistosomiasis. Unfortunately, it exhibits low oral bioavailability which can compromise its efficacy. Nanostructures showed promising potential to overcome this problem. Accordingly, the aim of this study was to investigate the effect of niosomal encapsulation of PZQ o...

Olmesartan medoxomil (Olm) and hydrochlorothiazide (HCTZ) are fixed dose combination (FDC) for treatment of hypertension. They have hydrogen bonding sites and may interact during co-processing. The consequences of such interaction are not clear. This study investigated the possibility of this interaction during co-processing. The research was exten...

BCS class III drugs suffer from limited intestinal absorption due to high hydrophilicity and low intestinal permeability. This research was undertaken in order to examine the effect of enhancing the net water influx in the gastrointestinal tract on the oral absorption of ranitidine HCl, atenolol, and acyclovir sodium as model BCS class III drugs us...

The aim was to optimize eugenol microemulsion for transdermal delivery of indomethacin (model drug). Pseudo-ternary phase diagrams were constructed using Tween 40 (surfactant) in presence and absence of ethanol or propylene glycol (PG) as co-surfactants. Microemulsion formulations containing eugenol at 10, 20 and 30% w/w with 60% w/w of surfactant...

Objectives The aim of this research was to assess regional difference in the intestinal absorption of ranitidine HCl as an indicator for the potential effect of P‐glycoprotein (P‐gp) efflux transporters. Methods In situ rabbit intestinal perfusion was used to investigate absorption of ranitidine HCl, a substrate for P‐gp efflux from duodenum, jeju...

Background Melasma is a common cause of cosmetic disfigurement in the face. This facial hyperpigmentation leads to many psychological problems. It is difficult to be treated and has a high rate of recurrence. Objective The aim of this study was to evaluate and compare the efficacy of topical tranexamic acid 5% versus topical flutamide 1% in the tre...

Objective: The main objective of this study was to investigate the potential of in situ crystallization of indomethacin, in presence or absence of hydrophilic materials, to improve drug dissolution with the goal of developing fast disintegrating tablets. Methods: Indomethacin crystals were prepared by bottom up approach. Water containing hydrophili...

The fluidity of vesicular membrane affects vesicular transdermal drug delivery. Essential oils can be located in vesicular membrane imparting flexibility and influencing transdermal delivery. Accordingly, the objective was to investigate the effect of incorporation of essential oils in niosomes on felodipine transdermal delivery. Rigid niosomes com...

Vitiligo is a skin disease characterized by depigmentation disorders due to lack of melanin production. Piperine, an alkaloid extracted from black piper, is active in melanocytes proliferation. To achieve this, the drug has to reach the melanocytes which exist in the deep layer of the epidermis. Higher drug concentration can be obtained after appli...

Peceol containing niosomes (peceosomes) have been shown to widen absorption window of acidic drugs. However, the relationship between drug release and intestinal absorption is not clear. Accordingly, the objective was to probe peceosomes for enhancing intestinal absorption of glibenclamide with the goal of correlating drug release with intestinal a...

The aim of this study was to develop floating microspheres for gastroretentive delivery of clarithromycin for eradication of Helicobacter pylori. The microspheres were prepared by solvent evaporation using ethyl cellulose (EC) at different weight ratio with clarithromycin with hydroxypropyl methyl cellulose (HPMC E5) acting as secondary polymer. Th...

Niosomes have been claimed to enhance intestinal absorption and to widen the absorption window of acidic drugs. This was reported after monitoring the intestinal absorption in situ. Accordingly, the aim of this work was to investigate the effect of niosomal encapsulation on intestinal absorption and oral bioavailability of nateglinide. This was con...

Background: Alopecia areata (AA) is one of the most common causes of localized hair loss. There is no universally proven therapy that induces and sustains remission of hair growth in AA. Objective: To compare the efficacy and safety of topical latanoprost, minoxidil and betamethasone valerate on hair growth in patients with AA. Patients and methods...

Breaching the barrier nature of the skin is the main strategy to enhance transdermal drug delivery. To achieve this, researchers employed different strategies developing alternative transdermal drug delivery systems. On doing this, minor attention was given to the method of application which can affect the integrity of the skin as well as the natur...

Objective: The aim of this work was to investigate the potential of controlled precipitation of flurbiprofen on solid surface, in presence or absence of hydrophilic polymers, as a tool for enhnaced dissolution rate of the drug. The work was extended to develop rapidly disintegrated tablets. Significance: This strategy provide simple technique fo...

p class="MsoNormal" style="margin-top: 6.0pt; margin-right: 0in; margin-bottom: 6.0pt; margin-left: 0in; text-align: justify; line-height: 97%;"> Objective: The aim of this work was to determine the intestinal membrane transport parameters of eprosartan mesylate (EM) and to investigate self-nano emulsifying drug delivery systems (SNEDDS) and inclus...

Nateglinide is a non-sulphonylurea which was approved for treatment of type II diabetes mellitus. Its pH dependent slow dissolution resulted in variable oral bioavailability. This work presents Co-crystallization as a strategy for enhanced dissolution rate of nateglinide. The study was extended to investigate the effect of this dissolution enhancem...

Amiodarone is antihypertensive drug with variable bioavailability following oral administration due to poor solubility and pre-systemic metabolism. Accordingly, the study strategy was to enhance the dissolution rate of the drug by solid dispersion (SD) and surface solid dispersion (SSD) techniques, with optimum formulations being developed as fast...

Background/aim: The increasing number of multidrug-resistant (MDR) bacteria and the need to synthesize new antimicrobials, nanoparticles have attracted interest in the scientific community. This study aimed to evaluate the synergistic effect of nanoparticles with some antibiotics against MDR pathogenic bacteria.ar

Mixed micelles provide promising strategy for enhancing dissolution and permeability of drugs. However, their fluid nature limited the stability of the loaded drug and hindered the development of stable oral dosage form. Accordingly, the objective was to develop solid self dispersing mixed micelle forming systems (MMFS) for enhanced dissolution and...

Dissolution enhancement is a promising strategy for improving drug bioavailability. Co-crystallization of drugs with inert material can help in this direction. The benefit will become even greater if the inert material can form co-crystal while maintaining its main function as excipient. Accordingly, the objective of the current study was to invest...

Liquisolid formulation involves dissolution or dispersion of the drug in a liquid before formulation of solid dosage form using solid adsorbent as a carrier. The liquid component usually utilizes simple solvent system. Self emulsifying liquids can provide another alternative liquid for enhanced dissolution. The objective of this work was to develop...

Objective: The aim of this study was to enhance the dissolution rate of hydrochlorothiazide (HCTZ). Methods: Binary solid dispersions (SDs) of HCTZ with increasing weight ratios of poloxamer 407, polyethylene glycol 6000 (PEG 6000) or gelucire 50/13 were prepared by solvent evaporation technique. The solid dispersions were deposited on the surface...