Increase Drug Absorption Research Articles

The Particle Drifting Effect: A Combined Function of Colloidal and Drug Properties.

The particle drifting effect, where nanosized colloidal drug particles overcome the diffusional resistance of the aqueous boundary layer adjacent to the intestinal wall and increase drug absorption rates, is drawing increasing attention in pharmaceutical research. However, mechanistic understanding and accurate prediction of the particle drifting effect remain lacking. In this study, we systematically evaluated the extent of the particle drifting effect affected by drug and colloidal properties, including the size, number, and type of the moving species using biphasic diffusion experiments combined with computational fluid dynamics simulations and mass transport analyses. The results showed that the particle drifting effect is a sequential reaction of particle dissolution/dissociation in the diffusional boundary layer, followed by absorption of the free drug. Therefore, factors affecting the rate-limiting step, which can be either process or both under different circumstances, alter the particle drifting effect. Experimental results also agree with the theory that the particle dissolution rate is dependent on particle size, concentration, and drug solubility. In addition, rapid bile micelle dissociation and bile salt absorption facilitated drug absorption by the particle drifting effect. Our findings explain the highly dynamic nature of the particle drifting effect and will contribute to rational formulation development and better bioavailability prediction for formulations containing colloidal particles.

Enhancement of Oral Bioavailability of Protein and Peptide by Polysaccharide-based Nanoparticles.

Oral drug delivery is a prevalent and cost-effective method due to its advantages, such as increased drug absorption surface area and improved patient compliance. However, delivering proteins and peptides orally remains a challenge due to their vulnerability to degradation by digestive enzymes, stomach acids, and limited intestinal membrane permeability, resulting in poor bioavailability. The use of nanotechnology has emerged as a promising solution to enhance the bioavailability of these vital therapeutic agents. Polymeric NPs, made from natural or synthetic polymers, are commonly used. Natural polysaccharides, such as alginate, chitosan, dextran, starch, pectin, etc., have gained preference due to their biodegradability, biocompatibility, and versatility in encapsulating various drug types. Their hydrophobic-hydrophilic properties can be tailored to suit different drug molecules.

The effect of emulgel preparation on the stability of Kojic acid in the topical anti-hyperpigmentation products.

The emulgel, a novel drug delivery system, merges emulsion and gel, offering advantages like enhanced stability, precise control over drug release kinetics, and increased drug absorption compared to emulsions alone. Kojic acid (KA) demonstrates potent inhibition of the tyrosinase enzyme, a crucial player in the melanin synthesis pathway. The main objective of this experimental study is to formulate KA within an emulgel framework and assess its stability under various environmental conditions. One percent of KA emulgel and 1% simple gel, serving as the control product, were supplemented with varying concentrations of sodium metabisulfite (SMBS) for its antioxidant properties. The formulations were segregated into four groups and subjected to diverse maintenance and stress conditions over a three-month period. Monthly evaluations of physicochemical alterations were conducted, initially employing digital photography, followed by the extraction of KA and subsequent quantification of its concentration through high performance liquid chromatography (HPLC). The best formulations for retaining KA among the prepared ones were the 0.25% SMBS KA emulgel and the 0.1% SMBS KA simple gel, capable of retaining 86% and 76% of the initial KA content under stress conditions, respectively (p < 0.0001). Regarding to this study, ideal storage condition for KA emulgel and simple gel is in the refrigerator temperatures. Moreover, optimal SMBS concentrations for stability enhancement are 0.25% for emulgel and 0.1% for the simple gel. A significant statistical difference was observed between refrigerated emulgel and simple gel in the retention of KA in the presence of optimum concentration of antioxidants (p < 0.0001).

Preparation of Hirudin-Loaded Chitosan/Polycaprolactone Bowl-Shaped Particles and an Application for a Drug Delivery System

Atherosclerosis, a disease that mainly affects human blood vessels, can cause various cerebral ischaemic diseases such as coronary heart disease and peripheral arterial disease. However, conventional drugs for the treatment of atherosclerosis have the disadvantages of low bioavailability and high toxicity. Bowl-shaped particles not only have the excellent properties of traditional spherical particles, such as improved drug distribution, increased drug absorption, reduced drug toxicity and side effects, but also are easier to circulate in the blood for a long time, have reduced immune rejection and have a larger specific surface area. Chitosan/polycaprolactone bowl-shaped particles were prepared via electrostatic spraying, and the effects of precursor solution concentration and polymer ratio on particle morphology were investigated. Chitosan/polycaprolactone composite bowl-shaped particles containing hirudin were prepared under optimal parameters for sustained anticoagulation. The anticoagulant molecules of hirudin could be continuously released from the composite scaffold as the bowl particles degraded. The biocompatibility and haemocompatibility of the composite particles were assessed using mouse glial cells and rabbit blood, and the results showed that the cell viability of the drug-loaded particles was overall above 90% and the haemolysis rate was below 2%. By controlling the release rate of hirudin, bowl-shaped particles can achieve a long-term anticoagulant drug delivery system and have wider application potential as a novel blood contact material.

Cancer Pharmacology Advances: Fundamentals, Combination, Imagery, Shipment and Therapeutic Applications

Cancer continues to be a major health issue worldwide, necessitating creative solutions to medication production and therapy techniques. It delves into the concepts of cancer drug activity, mixtures of drugs, imaging of molecules, delivery of medications, the interaction between medications, clinical utility and use, and the place of cancer medications across the procedure for discovering and developing drugs. Cancer therapy assumptions serve as the cornerstone for treatment methods. This understanding contributes directly to the intelligent planning of focused medicines, which aim to deliberately interrupt these channels while minimizing outside-target consequences and adverse reactions. Genome and transcriptomic studies have supplied a lot of understanding to aid in inventing personalized treatment techniques in cancer treatment. Cancer pharmaco has been transformed by molecular imaging tools that provide immediate visualization of medication action in the tumour ecosystem. Investigators can monitor medication transportation, pharmaceutical kinetics, and therapeutic using PET and MRI, as well as other approaches, supporting personalized regimens for therapy. Cancer medication means of distribution have emerged in order to increase drug absorption, decrease poisoning, or enhance directed drug administration. Creative ideas for drug delivery techniques that have shown interest in clinical studies include micron-sized particles of liposomes and antibody-drug conjugates. In cancer survivors, extensive toxicological research and computer modelling are critical in discovering likely interactions and guiding choosing therapy and administration. Cancer pharmacology's clinical significance and applications span from test to bed.

Formulation development and evaluation of nasal in situ gel of promethazine hydrochloride

Objective The present work aims to develop mucoadhesive thermosensitive nasal in situ gel for Promethazine hydrochloride using quality by design (QbD) approach. It can reduce nasal mucociliary clearance (MCC) and increase residence of the drug on nasal mucosa. This might increase drug absorption to improve bioavailability of the drug as compared to oral dosage form. Significance Promethazine hydrochloride is an antiemetic drug administered by oral, parenteral and rectal routes. These routes have poor patient compliance or low bioavailability. Nasal route is a better alternative as it has large surface area, high drug absorption rate and no first pass effect. Its only limitation is short drug retention time due to MCC. By formulating a mucoadhesive in situ gel, the MCC can be reduced, and drug absorption will be prolonged. Thus, improving bioavailability. Method In-situ gel was prepared by cold method having material attributes as concentration of Poloxamer 407 (X1) as gelling agent and hydroxypropyl methyl cellulose K4M (X2) as mucoadhesive agent. Critical Quality Attributes (CQA) were gelation temperature, mucoadhesive force and ex-vivo diffusion. Central composite design (CCD) was adopted for optimization. Result Optimized formulation satisfied all the CQA significant for nasal administration. Moreover, the formulation was found to be stable in accelerated stability studies for 3 months. Conclusion It can be concluded that since the drug can easily permeate through nasal mucosa and can gain access directly in the brain without undergoing first pass metabolism along with increased residence due to mucoadhesion, mucoadhesive in situ gel has potential to increase drug bioavailability.

In vitro identification of decreased function phenotype ABCG2 variants

Reduced activity of efflux transporter ABCG2, caused e.g., by inhibition or decreased function genetic variants, can increase drug absorption and plasma levels. ABCG2 has one clinically significant single nucleotide variant Q141K (c.421C>A), which leads to decreased protein levels and transport activity. In addition to Q141K, ABCG2 has over 500 rare (<1% minor allele frequency) nonsynonymous variants, but their functionality remains unknown. We studied the transport activity and abundance of 30 rare ABCG2 variants. The variants were transiently expressed in HEK293 cells. Transport activity and protein abundance were measured from inside-out crude membrane vesicles. Results were normalised to the reference ABCG2, while Q141K was used to categorise variants into decreased and normal function phenotypes based on their apparent transport activity. Fourteen variants (G80E, D128V, T434M, Q437R, C438R, C438W, C438Y, L479S, P480L, S486N, T512N, S519P, G553D and K647E) had similar or lower apparent transport activity than Q141K and thus were categorised as having a decreased function phenotype. Protein abundance could not explain all of the observed changes in transport activity: Only six variants (D128V, Q437R, C438R, S519P, G553D, and K647E) had similar or lower abundance compared to Q141K. The decreased function variants may increase systemic drug exposure and therefore cause interindividual variability in pharmacokinetics. In the future, in vitro phenotype classification may help to design personalised drug treatments.

In-vitro and In-vivo Characterization of Anti-Onychomycotic Transungual patches - A Systematic Review

Transungual drug delivery systems distribute therapeutic agents through the human nail, a unique way for delivering medications for nail disorders caused by fungal infections. The human nail is a hydrophilic barrier made up of keratinized cells that cover the nail bed and matrix underneath. For nail diseases, the systemic or oral mode of drug delivery reduces the drug's potency at the site of action. To achieve longer contact duration at the application site, it is necessary to increase drug absorption to the nail unit. The primary goal of this review paper is to provide an overview of characterization studies on physicochemical characteristics; in-vitro and in-vivo approaches for transungual drug delivery to treat nail fungal infections using medicated nail patches. However, in order to acquire a wide overview of the characterization elements of this rapidly increasing multidisciplinary field of study, a number of articles and technical studies dealing with nail patches were investigated. It also included the methodology employed in the characterization studies, as well as the implications for process design.

A Micro-In-Macro Gastroretentive System for the Delivery of Narrow-Absorption Window Drugs.

A micro-in-macro gastroretentive and gastrofloatable drug delivery system (MGDDS), loaded with the model-drug ciprofloxacin, was developed in this study to address the limitations commonly experienced in narrow-absorption window (NAW) drug delivery. The MGDDS, which consists of microparticles loaded in a gastrofloatable macroparticle (gastrosphere) was designed to modify the release of ciprofloxacin, allowing for an increased drug absorption via the gastrointestinal tract. The prepared inner microparticles (1-4 µm) were formed by crosslinking chitosan (CHT) and Eudragit® RL 30D (EUD), with the outer gastrospheres prepared from alginate (ALG), pectin (PEC), poly(acrylic acid) (PAA) and poly(lactic-co-glycolic) acid (PLGA). An experimental design was utilized to optimize the prepared microparticles prior to Fourier Transition Infrared (FTIR) spectroscopy, Scanning Electron Microscopy (SEM) and in vitro drug release studies. Additionally, the in vivo analysis of the MGDDS, employing a Large White Pig model and molecular modeling of the ciprofloxacin-polymer interactions, were performed. The FTIR results determined that the crosslinking of the respective polymers in the microparticle and gastrosphere was achieved, with the SEM analysis detailing the size of the microparticles formed and the porous nature of the MGDDS, which is essential for drug release. The in vivo drug release analysis results further displayed a more controlled ciprofloxacin release profile over 24 h and a greater bioavailability for the MGDDS when compared to the marketed immediate-release ciprofloxacin product. Overall, the developed system successfully delivered ciprofloxacin in a control-release manner and enhanced its absorption, thereby displaying the potential of the system to be used in the delivery of other NAW drugs.

Acute Toxicity of Self-Nanoemulsifying Drug Delivery System of Ipomoea reptans Poir Leaves Extract on Female Wistar Rats

Ipomoea reptans Poir has many health benefits, such as decreasing blood glucose and as an antioxidant. Self-nano emulsifying drug delivery systems (SNEDDS) are an innovation in pharmaceutical technology that minimizes drug molecules and maximizes surface area, thus increasing drug absorption. This study aimed to investigate SNEDDS of I. reptans acute toxicity in female Wistar rats. An acute toxicity test was done using a limit test of OECD 423. Female Wistar rats were divided into control and treatment groups, with three animals for each group being used per step. No animals died after they were given SNEDDS of I. reptans leaves extract at a dose of 2000 mg/kg. No toxic effect was detected at clinical examination and histopathology of the organ. SNEDDS of I. reptans leaves extract had an LD50 cut-off value of 5000 mg/kg.

Recent Advances in Intranasal Liposomes for Drug, Gene, and Vaccine Delivery.

Liposomes are safe, biocompatible, and biodegradable spherical nanosized vesicles produced from cholesterol and phospholipids. Recently, liposomes have been widely administered intranasally for systemic and brain delivery. From the nasal cavity, liposome-encapsulated drugs and genes enter the systemic circulation primarily via absorption in the respiratory region, whereas they can be directly transported to the brain via the olfactory pathway. Liposomes can protect drugs and genes from enzymatic degradation, increase drug absorption across the nasal epithelium, and prolong the residence time in the nasal cavity. Intranasal liposomes are also a potential approach for vaccine delivery. Liposomes can be used as a platform to load antigens and as vaccine adjuvants to induce a robust immune response. With the recent interest in intranasal liposome formulations, this review discusses various aspects of liposomes that make them suitable for intranasal administration. We have summarized the latest advancements and applications of liposomes and evaluated their performance in the systemic and brain delivery of drugs and genes administered intranasally. We have also reviewed recent advances in intranasal liposome vaccine development and proposed perspectives on the future of intranasal liposomes.

Discovery of benzyloxyphenyl- and phenethylphenyl-imidazole derivatives as a new class of ante–drug type boosters

Although cytochrome P450 3A4 (CYP3A4) inhibitors are used as boosters to increase drug absorption, the inhibition of CYP3A4 activity may affect the metabolism of other co-administered drugs. Therefore, we screened for and developed a new class of boosters to improve the oral availability of drugs. We identified benzyloxyphenyl imidazole and phenethylphenyl imidazole derivatives as new types of CYP3A4 inhibitors. Among the compounds synthesized, an ester 5c was found to inhibit CYP activity and the compound 5c was gradually converted to an inactive metabolite 5d under physiological conditions, indicating that the ester 5c may represent a novel ante-drug type booster.

Recent Development in Floating Drug Delivery System: An Overview

Floating medicines work well to increase drug absorption in the stomach. On the basis of current literature, a drug for a novel drug delivery system (NDDS) is established to explicate the floating drug delivery system (FDDS). The most recent FDDS progress involves the formulation as well as physiological aspects that may affect gastric retention and formulation. This review also discusses certain ways of producing a floating system, as well as evaluation methods, characterization, and classification for the FDDS pharmaceutical dosage form. By overcoming physiological hurdles such as short stomach residence times and unexpected gastric emptying times, scientific and technological achievements have been made in the study and development of controlled-release oral drug delivery systems in recent years. So, in general, float dose systems are key technological medication delivery systems that have a stomach-retentive nature and provide a variety of options. Floating drug delivery systems (FDDS), also known as hydro dynamically balanced systems (HBS), swelling and expanding systems, polymeric bio-adhesive systems, modified-shape systems, high-density systems, and other delayed gastric emptying devices are now used to extend the GRT. The latest technological breakthroughs of FDDS, including patented delivery methods and commercialized products, are covered in this study, as well as their advantages and future possibilities for oral controlled drug administration.&#x0D; Keywords- A novel drug gastrointestinal tract, types of FDDS, gastric residence time, evaluation of FDDS

Noninvasive Drug Delivery System Progress in Protein and Peptide Delivery

Protein and peptide drugs have tremendous therapeutic potential, and their usage in the treatment of various severe diseases has revolutionized the fields of pharmaceuticals and biotechnology. For successful therapeutic effects, several efforts have been made to deliver protein/peptide drugs through various routes of administration. Parenteral and nonparenteral drug deliveries are regarded as significant routes of drug absorption. However, there is a need to improve nonparenteral drug delivery systems (DDSs) through subsequent routes, including buccal, pulmonary, oral, ocular, transdermal, and nasal routes to increase drug absorption effectively. The study evaluated various DDS routes proposed for the distribution of proteins and peptides in terms of both parenteral and nonparenteral delivery systems. For this purpose, numerous research articles were searched from the year 2000 to 2021 using search engines such as PubMed, Google Scholar, Medline, ISI Web of Knowledge, and Bioline International while applying different keywords such as “protein and peptide drugs,” “drug delivery systems,” “parenteral and nonparenteral routes of drug delivery,” and “physicochemical barriers.” The invasive/parenteral routes have several limitations associated with drug delivery, such as poor patient compliance and the pain and discomfort associated with these routes inconvenience in treating the pediatric population. The oral route is one of the most convenient routes of noninvasive or nonparenteral drug administration; here, no pain and discomfort arise, thus helping in maintaining higher patient compliance or acceptance. The other routes of administration of proteins and peptides through buccal, intranasal, pulmonary, transdermal, rectal, and ocular routes have also been showing successful results. The success of the therapeutics is strongly influenced by the differential delivery of the targeted antigen, the choice of targeting protein or peptide, and the drug-release characteristics of the linker used. Furthermore, there should be an improvement in nonparenteral DDSs so that the drugs might be administered appropriately.

Phytochemical Screening and Emulgel Formulation of Jernang Resin Extract (Daemonorops Draco (Willd) Blume)

Objective: Daemonorops draco (Willd) Blume is a plant that produces jernang, which is a red resin that sticks to the outer skin of the fruit. Also known as dragon's blood, it is used as a traditional medicine for wound healing, anti-diarrhea, etc. as a natural coloring agent. Emulgel is an emulsion that contains a gel base in a certain ratio. Emulgel has the advantages of increasing drug absorption, easy to apply and more comfortable, not sticky on the skin. This study aims to determine the class of secondary metabolites contained in jernang in the form of simplicia and their extracts and to make jernang resin extract emulgel preparations that can be used as wound medicine.&#x0D; Method: Jernang simplicia collected by dry method. The extract was made by maceration using 96% ethanol solvent, separating the solvent using a rotary evaporator and concentrating it on a water bath. Phytochemical screening was carried out on simplicia and extracts. The emulsion formulation of jernang resin extract was made in three formulas with various levels of extracts P1 (2.5%), P2 (5%) and P3 (7.5%), using Tween 80 and Isopropyl myristate (IPA) as surfactants and oil phase, and 1% Carbopol as a gel base, then the emulgel was made with a ratio of emulsion and gel base of 4: 1 so that the variations of the extract were made into three formulas P4 (2%), P5 (4%) and P6 (6%)&#x0D; RESULTS: The results of phytochemical screening showed that jernang simplicia contained flavonoid, glycoside and saponin compounds. Also compounds that are non-polar, namely steroids / triterpenoids. Whereas in the form of the extract it contains flavonoid class compounds, this is because the 96% ethanol solvent is semi-polar so that the compounds contained in the ethanol extract are polar compounds, namely flavonoids which are the largest content of compounds in jernang. Jernang P4 extract emulgel (2%) organoleptically has the best physical appearance, has the characteristics of a thick, slightly clear consistency, brownish red color, has a distinctive smell of jernang mixed with the aroma of Tween 80, and is homogeneous.&#x0D; Conclusion: Based on the test results, it can be concluded that in the form of jernang simplicia, it contains polar compounds (flavonoids, glycosides and saponins) and non-polar (steroid / terponoid groups) and in the form of jernang resin extract contains flavonoid class compounds. Organoleptically, the jernang resin extract emulgel with a content of 2% (P4) is the best formula compared to other formulas.&#x0D;

Recent Advancements in Nanotechnology for Oral Cancer: a Review

Background: Oral cancer is the life threatening disease causing mortality. The majority of chemotherapeutic anticancer agents are toxic to healthy tissues, have poor bioavailability and affect the quality of life of the patients. Objective: The main challenge in the treatment of oral cancer is the effective and safe delivery of chemotherapeutic anticancer drugs. This present review deals with the recent advancement in the nanotechnologies and its probable applications in the oral cancer treatment. Methods: This review includes a gist of suitable literature. Results: Nanotechnology brings novel methodologies or modifications in current anticancer therapies to improve individual wellbeing and survival. Conclusion: Nanotechnology put forward the potential of increasing the efficacy of the therapy and targeted drug delivery, which in turn increase drug absorption and bioavailability at the site of tumour. Different nanocarriers include liposomes, polymeric nanoparticles, inorganic nanoparticles, combinational (polymeric- inorganic) nanoparticles, magnetic nanoparticles, nanolipids, hydrogels, dendrimers and polymeric micelles. This review confers development of new drug delivery approaches for effective therapeutic outcomes and abating the toxicity to healthy tissues.

Self - Emulsifying Drug Delivery System: A Novel Approach for Oral Delivery of Poorly Water Soluble Drugs

Self nano emulsifying drug delivery systems (SNEDDs) gained much attention in the last decades since, such systems considered one of the most favorable and efficient approaches to enhance solubility, increase drug absorption and hence, enhance its oral bioavailability of poorly water soluble (lipophilic) drug moieties. Owing to their unique properties and advantages over the other conventional dosage forms, many literatures investigate the change physicochemical properties, pharmacokinetic and pharmacodynamics of self emulsifying formulation compared to both pure drug and its conventional dosage form and always reported significant improvement using SNEDDs. This review discus the composition, advantages and mechanism of action of liquid SNEDDs and some techniques used for solidification of liquid formulations to overcome its drawbacks.

AN UPDATE ON BIO-POTENTIATION OF DRUGS USING NATURAL OPTIONS

The objective of this review is to put a light on the benefits of bio-enhancers and their role in developing a proper drug delivery system having improved therapeutic action and least drawbacks. As medical science is developing fast and there is a considerable increase in the development of new drugs with many therapeutic activities, but having lots of side effects, less in vivo action, or are very costly. These drawbacks create an enormous demand for use of bio-enhancers to reduce the dose required of the active ingredients and provide a suitable condition for their actions. There are vast nature-derived bio-enhancers originated from plants or other natural sources, used to a great extent as they show high activity and have very little or no adverse effects. Bio-enhancers increase bioavailability in various ways such as by increasing drug absorption, decreasing drug metabolism, and by other methods, which helps the drug having low bioavailability but the good therapeutic potential to show its effect fast. The concept of bio-enhancers developing increasingly in modern medicine but in reality, was there and well explained in Ayurveda texts with various herbal drugs such as piperine, quercetin, genistein, naringin and some non-herbal compounds such as cow urine distillate, and Capmul. Along with these nature-derived bio-enhancers and the new techniques such as liposomes, nanoparticles, transferosomes, and ethosomes resulted in the successful modification of suitable dosage forms. The concept of bioenhancers and their application is a great tool which can lead to a excellent development of medical science.

Biomimetic micellar mesoporous silica xerogel performs superior nitrendipine dissolution, systemic stability and cellular transmembrane transport.

To combine the advantages of micelles and biomimetic silica materials, biomimetic micellar mesoporous silica xerogel (BM-SX) was initially established, biomimetic silica xerogel (B-SX) was also studied as control and nitrendipine (NDP) was taken as model drug. The content mainly focused on drug dissolution, systemic stability and cellular transmembrane transport of NDP loaded B-SX and NDP loaded BM-SX. With extra mesopores formed due to HPMC E50 micelles, the mean pore diameter, surface area and pore volume of BM-SX were all larger than B-SX. After loading NDP into the two carriers, crystal NDP changed to amorphous phase, leading to enhanced NDP dissolution. BM-SX presented superior abilities not only for its higher drug dissolution compared to B-SX but also for its capacity in remaining high amorphous drug phase and therefore no drug dissolution reduction can be observed. The dynamic contact angle result confirmed the strong power of HPMC E50 micelles in maintaining amorphous NDP in the carrier to improve high systemic stability. Both B-SX and BM-SX could increase drug absorption permeability and exert function as drug efflux inhibitor to inhibit the efflux effect of p-gp drug pump and promote NDP absorption and transport, and BM-SX was superior owing to micelles in the system.

Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization.

In the past decade, pharmaceutical nanotechnology has proven to be a promising alternative for improving the physicochemical and biopharmaceutical features for conventional pharmaceutical drug formulations. The goal of this study was to develop, characterize, and evaluate the in vitro and in vivo release of the model drug carbamazepine (CBZ) from two emulsified formulations with different droplet sizes (coarse and nanometric). Briefly, oil-in-water emulsions were developed using (i) Sacha inchi oil, ultrapure water, TweenTM 80, and SpanTM 80 as surfactants, (ii) methyl-paraben and propyl-paraben as preservatives, and (iii) CBZ as a nonpolar model drug. The coarse and nanometric emulsions were prepared by rotor–stator dispersion and ultra-high-pressure homogenization (UHPH), respectively. The in vitro drug release studies were conducted by dialysis, whereas the in vivo drug release was evaluated in New Zealand breed rabbits. The results showed that nanoemulsions were physically more stable than coarse emulsions, and that CBZ had a very low release for in vitro determination (<2%), and a release of 20% in the in vivo study. However, it was found that nanoemulsions could significantly increase drug absorption time from 12 h to 45 min.